标签归档：calp

CALP1 TFA

发表于由

CALP1 TFA;

CALP1 TFA 是一种钙调蛋白 (CaM) 激动剂 (Kd 为 88 µM)，与 CaM EF-hand/Ca2+ 结合位点结合。CALP1 TFA 通过抑制钙通道 (calcium channel) 的开放来阻止钙的流入和凋亡 (IC50 为 44.78 µM)。CALP1 TFA 阻止谷氨酸受体 ( glutamate receptor channels) 通道，并阻止存储操作的非选择性阳离子通道。CALP1 TFA 激活 CaM 依赖性磷酸二酯酶 (phosphodiesterase) 活性。

CALP1 TFAamp;;

CALP1 TFA Chemical Structure

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

生物活性

CALP1 TFA is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca2+-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity[1][2][3][4].

IC50 Target

Kd: 88 µM (Calmodulin)[4]
分子量

956.10

Formula

C42H76F3N9O12
Sequence

Val-Ala-Ile-Thr-Val-Leu-Val-Lys
Sequence Shortening

VAITVLVK
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. R Houtman, et al. Attenuation of very late antigen-5-mediated adhesion of bone marrow-derived mast cells to fibronectin by peptides with inverted hydropathy to EF-hands. J Immunol. 2001 Jan 15;166(2):861-7.

    [2]. R Ten Broeke, et al. Calcium sensors as new therapeutic targets for airway hyperresponsiveness and asthma. FASEB J. 2001 Aug;15(10):1831-3.

    [3]. M K Manion, et al. A new type of Ca(2+) channel blocker that targets Ca(2+) sensors and prevents Ca(2+)-mediated apoptosis. FASEB J. 2000 Jul;14(10):1297-306.

    [4]. M Villain, et al. De novo design of peptides targeted to the EF hands of calmodulin. J Biol Chem. 2000 Jan 28;275(4):2676-85.

CALP1

发表于由

CALP1;

CALP1 是一种钙调蛋白 (CaM) 激动剂 (Kd 为 88 µM)，与 CaM EF-hand/Ca2+ 结合位点结合。CALP1 通过抑制钙通道 (calcium channel) 的开放来阻止钙的流入和凋亡 (IC50 为 44.78 µM)。CALP1 阻止谷氨酸受体 ( glutamate receptor channels) 通道，并阻止存储操作的非选择性阳离子通道。CALP1 激活 CaM 依赖性磷酸二酯酶 (phosphodiesterase) 活性。

CALP1amp;;

CALP1 Chemical Structure

CAS No. : 145224-99-3

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

生物活性

CALP1 is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca2+-binding site. CALP1 blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity[1][2][3][4].

IC50 Target

Kd: 88 µM (Calmodulin)[4]
分子量

842.08

Formula

C40H75N9O10
CAS 号

145224-99-3
Sequence

Val-Ala-Ile-Thr-Val-Leu-Val-Lys
Sequence Shortening

VAITVLVK
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. R Houtman, et al. Attenuation of very late antigen-5-mediated adhesion of bone marrow-derived mast cells to fibronectin by peptides with inverted hydropathy to EF-hands. J Immunol. 2001 Jan 15;166(2):861-7.

    [2]. R Ten Broeke, et al. Calcium sensors as new therapeutic targets for airway hyperresponsiveness and asthma. FASEB J. 2001 Aug;15(10):1831-3.

    [3]. M K Manion, et al. A new type of Ca(2+) channel blocker that targets Ca(2+) sensors and prevents Ca(2+)-mediated apoptosis. FASEB J. 2000 Jul;14(10):1297-306.

    [4]. M Villain, et al. De novo design of peptides targeted to the EF hands of calmodulin. J Biol Chem. 2000 Jan 28;275(4):2676-85.

CALP3 TFA

发表于由

CALP3 TFA;

CALP3 TFA 是一种类似于 Ca2+ 的肽，是有效的 Ca2+ 通道阻滞剂，可激活 Ca2+ 结合蛋白的 EF 手。CALP3 TFA 可以通过调节钙调蛋白 (CaM)，Ca2+ 通道和泵的活性来模拟增加的 [Ca2+]i。CALP3 TFA 具有控制诸如艾滋病或由于缺血引起的神经元丢失等疾病中细胞凋亡的潜力。

CALP3 TFAamp;;

CALP3 TFA Chemical Structure

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

生物活性

CALP3 TFA, a Ca2+-like peptide, is a potent Ca2+ channel blocker that activates EF hand motifs of Ca2+-binding proteins. CALP3 TFA can functionally mimic increased [Ca2+]i by modulating the activity of Calmodulin (CaM), Ca2+ channels and pumps. CALP3 TFA has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia[1][2].

IC50 Target[1][2]

Ca2+

;

体外研究
(In Vitro)

CALP3 TFA (50, 100, 150, 200 μM) inhibits glutamate caused a large sustained increase in [Ca2+]i in a dose-dependent manner (IC50=37.25 μM) in Fura-2-loaded neuronal cultures[1].
CALP3 TFA (50, 100, 150, 200 μM) inhibits glutamate-induced cytotoxicity in a dose-dependent manner (IC50=50.97 μM) in cultured rat neocortical neurons. CALP3 TFA causes dose-dependent inhibition of apoptosis (IC50=33.41 μM)[1].
CALP3 TFA (100 μM) inhibits apoptosis induced by HIV gp120 and SAg in Human T cells[1].
CALP3 TFA (100 μM; 15 min pretreatment) reduces gossypol-induced necrosis and increases the fraction of live cells[2].
Cyclic-CALP3 is synthesized starting from Fmoc-Asp(PEG-PS)-OAl. Cyclic CALP3 is unable to inhibit Ca21 influx, and this peptide served as a negative control. Cyclic CALP3 does not inhibit the effect of glutamate[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

995.10

Formula

C46H69F3N10O11
Sequence Shortening

VKFGVGFK
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Manion MK, et al. A new type of Ca(2+) channel blocker that targets Ca(2+) sensors and prevents Ca(2+)-mediated apoptosis. FASEB J. 2000 Jul;14(10):1297-306.

    [2]. Ferdek PE, et al. BH3 mimetic-elicited Ca2+ signals in pancreatic acinar cells are dependent on Bax and can be reduced by Ca2+-like peptides. Cell Death Dis. 2017 Mar 2;8(3):e2640.

CALP2

发表于由

CALP2;

CALP2 是一种钙调蛋白 (CaM) 拮抗剂 (Kd 为 7.9 µM)，以亲和力结合 CaM EF-hand/Ca2+ 结合位点。CALP2 抑制 CaM 依赖性磷酸二酯酶 (phosphodiesterase) 活性并增加细胞内 Ca2+ 浓度。CALP2 有效抑制粘附和脱粒。CALP2 还是肺泡巨噬细胞的强激活剂。

CALP2amp;;

CALP2 Chemical Structure

CAS No. : 261969-04-4

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

CALP2 的其他形式现货产品:

CALP2 TFA

生物活性

CALP2 is a calmodulin (CaM) antagonist ( (Kd of 7.9 µM)) with high affinity for binding to the CaM EF-hand/Ca2+-binding site. CALP2 inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca2+ concentrations. CALP2 potently inhibits of adhesion and degranulation. CALP2 is also a strong activator of alveolar macrophages[1][2][3][4].

分子量

1357.70

Formula

C68H104N14O13S
CAS 号

261969-04-4
Sequence

Val-Lys-Phe-Gly-Val-Gly-Phe-Lys-Val-Met-Val-Phe
Sequence Shortening

VKFGVGFKVMVF
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. R Houtman, et al. Attenuation of very late antigen-5-mediated adhesion of bone marrow-derived mast cells to fibronectin by peptides with inverted hydropathy to EF-hands. J Immunol. 2001 Jan 15;166(2):861-7.

    [2]. R Ten Broeke, et al. Calcium sensors as new therapeutic targets for airway hyperresponsiveness and asthma. FASEB J. 2001 Aug;15(10):1831-3.

    [3]. Robert Ten Broeke, et al. Specific modulation of calmodulin activity induces a dramatic production of superoxide by alveolar macrophages. Lab Invest. 2004 Jan;84(1):29-40.

    [4]. M Villain, et al. De novo design of peptides targeted to the EF hands of calmodulin. J Biol Chem. 2000 Jan 28;275(4):2676-85.

CALP3

发表于由

CALP3; 纯度: 99.27%

CALP3 是一种类似于 Ca2+ 的肽，是有效的 Ca2+ 通道阻滞剂，可激活 Ca2+ 结合蛋白的 EF 手。CALP3 可以通过调节钙调蛋白 (CaM)，Ca2+ 通道和泵的活性来模拟增加的 [Ca2+]i。CALP3 具有控制诸如艾滋病或由于缺血引起的神经元丢失等疾病中细胞凋亡的潜力。

CALP3amp;;

CALP3 Chemical Structure

CAS No. : 261969-05-5

规格 价格 是否有货 数量
1 mg ￥1500 In-stock
5 mg ￥6000 In-stock
10 mg ￥9900 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

CALP3 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Membrane Transporter/Ion Channel Compound Library
  • Neuronal Signaling Compound Library
  • Anti-Cancer Compound Library
  • Neuroprotective Compound Library
  • Peptide Library

生物活性

CALP3, a Ca2+-like peptide, is a potent Ca2+ channel blocker that activates EF hand motifs of Ca2+-binding proteins. CALP3 can functionally mimic increased [Ca2+]i by modulating the activity of Calmodulin (CaM), Ca2+ channels and pumps. CALP3 has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia[1][2].

IC50 Target

Ca2+

;

体外研究
(In Vitro)

CALP3 (50, 100, 150, 200 μM) inhibits glutamate caused a large sustained increase in [Ca2+]i in a dose-dependent manner (IC50=37.25 μM) in Fura-2-loaded neuronal cultures[1].
CALP3 (50, 100, 150, 200 μM) inhibits glutamate-induced cytotoxicity in a dose-dependent manner (IC50=50.97 μM) in cultured rat neocortical neurons. CALP3 causes dose-dependent inhibition of apoptosis (IC50=33.41 μM)[1].
CALP3 (100 μM) inhibits apoptosis induced by HIV gp120 and SAg in Human T cells[1].
CALP3 (100 μM; 15 min pretreatment) reduces gossypol-induced necrosis and increases the fraction of live cells[2].
Cyclic-CALP3 is synthesized starting from Fmoc-Asp(PEG-PS)-OAl. Cyclic CALP3 is unable to inhibit Ca21 influx, and this peptide served as a negative control. Cyclic CALP3 does not inhibit the effect of glutamate[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

881.07

Formula

C44H68N10O9
CAS 号

261969-05-5
Sequence Shortening

VKFGVGFK
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

DMSO : 12.5 mg/mL (14.19 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.1350 mL 5.6749 mL 11.3498 mL
5 mM 0.2270 mL 1.1350 mL 2.2700 mL
10 mM 0.1135 mL 0.5675 mL 1.1350 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 1.25 mg/mL (1.42 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (1.42 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.25 mg/mL (1.42 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (1.42 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

    Solubility: ≥ 1.25 mg/mL (1.42 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (1.42 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Manion MK, et al. A new type of Ca(2+) channel blocker that targets Ca(2+) sensors and prevents Ca(2+)-mediated apoptosis. FASEB J. 2000 Jul;14(10):1297-306.

    [2]. Ferdek PE, et al. BH3 mimetic-elicited Ca2+ signals in pancreatic acinar cells are dependent on Bax and can be reduced by Ca2+-like peptides. Cell Death Dis. 2017 Mar 2;8(3):e2640.

CALP2 TFA

发表于由

CALP2 TFA; 纯度: 98.48%

CALP2 TFA 是一种钙调蛋白 (CaM) 拮抗剂 (Kd 为 7.9 µM)，以亲和力结合 CaM EF-hand/Ca2+ 结合位点。CALP2 TFA 抑制 CaM 依赖性磷酸二酯酶 (phosphodiesterase) 活性并增加细胞内 Ca2+ 浓度。CALP2 TFA 有效抑制粘附和脱粒。CALP2 TFA 还是肺泡巨噬细胞的强激活剂。

CALP2 TFAamp;;

CALP2 TFA Chemical Structure

规格 价格 是否有货 数量
5 mg ￥2000 In-stock
10 mg ￥3400 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

CALP2 TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Membrane Transporter/Ion Channel Compound Library
  • Metabolism/Protease Compound Library
  • Neuronal Signaling Compound Library
  • Reprogramming Compound Library
  • Anti-Alzheimer’s Disease Compound Library
  • Neurodegenerative Disease-related Compound Library
  • Anti-Colorectal Cancer Compound Library
  • Peptide Library

生物活性

CALP2 TFA is a calmodulin (CaM) antagonist (Kd of 7.9 µM) with high affinity for binding to the CaM EF-hand/Ca2+-binding site. CALP2 TFA inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca2+ concentrations. CALP2 TFA potently inhibits of adhesion and degranulation. CALP2 TFA is also a strong activator of alveolar macrophages[1][2][3][4].

分子量

1471.72

Formula

C70H105F3N14O15S
Sequence

Val-Lys-Phe-Gly-Val-Gly-Phe-Lys-Val-Met-Val-Phe
Sequence Shortening

VKFGVGFKVMVF
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro:;

DMSO : 50 mg/mL (33.97 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.6795 mL 3.3974 mL 6.7948 mL
5 mM 0.1359 mL 0.6795 mL 1.3590 mL
10 mM 0.0679 mL 0.3397 mL 0.6795 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.5 mg/mL (1.70 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.70 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (1.70 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (1.70 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.5 mg/mL (1.70 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.70 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. R Houtman, et al. Attenuation of very late antigen-5-mediated adhesion of bone marrow-derived mast cells to fibronectin by peptides with inverted hydropathy to EF-hands. J Immunol. 2001 Jan 15;166(2):861-7.

    [2]. R Ten Broeke, et al. Calcium sensors as new therapeutic targets for airway hyperresponsiveness and asthma. FASEB J. 2001 Aug;15(10):1831-3.

    [3]. Robert Ten Broeke, et al. Specific modulation of calmodulin activity induces a dramatic production of superoxide by alveolar macrophages. Lab Invest. 2004 Jan;84(1):29-40.

    [4]. M Villain, et al. De novo design of peptides targeted to the EF hands of calmodulin. J Biol Chem. 2000 Jan 28;275(4):2676-85.