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Pentagastrin(Synonyms: 五肽胃泌素 ICI-50123)

发表于由

Pentagastrin;(Synonyms: 五肽胃泌素; ICI-50123) 纯度: 98.02%

Pentagastrin (ICI-50123) 是胆囊收缩素 B (CCKB) 受体的选择性激动剂，IC50 为 11 nM。可增强胃粘膜对酸的防御机制，并保护胃粘膜免受损伤。

Pentagastrinamp;;(Synonyms: 五肽胃泌素; ICI-50123)

Pentagastrin Chemical Structure

CAS No. : 5534-95-2

规格 价格 是否有货 数量
10;mM;*;1 mL in DMSO ￥676 In-stock
5 mg ￥550 In-stock
10 mg ￥800 In-stock
25 mg ￥1600 In-stock
50 mg ￥2600 In-stock
100 mg ￥4400 In-stock
200 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

Pentagastrin 相关产品

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  • Drug Repurposing Compound Library Plus
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  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Neuronal Signaling Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Drug Repurposing Compound Library
  • Endocrinology Compound Library
  • Anti-COVID-19 Compound Library
  • NMPA-Approved Drug Library
  • Neurotransmitter Receptor Compound Library
  • FDA Approved amp; Pharmacopeial Drug Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Anti-Obesity Compound Library
  • Targeted Diversity Library
  • Rare Diseases Drug Library
  • Peptide Library

生物活性

Pentagastrin (ICI-50123) is a selective agonist of Cholecystokinin B (CCKB) receptor with an IC50 of 11 nM[1]. Pentagastrin enhances gastric mucosal defence mechanisms against acid and protects the gastric mucosa from experimental injury[2].

IC50 Target

IC50: 11 nM (CCKB receptor)[1]
体外研究
(In Vitro)

Cholecystokinin receptors on GH3 rat anterior pituitary cells have been characterised using radioligand binding and Ca2+ mobilisation. Competition curve with Pentagastrin (IC50 of 25 nM) is consistent with a population predominantly of CCKB receptors. The selective CCKB receptor agonist, Pentagastrin, (0.1 nM-100 μM) dose dependently increased intracellular Ca2+ with a maximal increase of 2.77-fold. Binding of 50 pM [125I]BHCCK to GH 3 cells is dose dependently inhibited by Pentagastrin IC50 of 45 nM. Response to a submaximal dose of the CCKB receptor agonist Pentagastrin (100 nM) was dose dependently blocked by the CCKB receptor antagonist L-365,260[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Pentagastrin (80 µg/kg/h; intravenous injection; male Sprague-Dawley rats) treatment protects rat gastric mucosa from acidified aspirin injury. Pentagastrin induces a hyperaemic response to luminal acid challenge, increases mucus gel thickness, and elevates intracellular pH (pHi) during acid challenge[2].

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

Animal Model: Male Sprague-Dawley rats (approximately 200 g)[2]
Dosage: 80 µg/kg/h
Administration: Intravenous injection
Result: Protected rat gastric mucosa from acidified aspirin injury. Induced a hyperaemic response to luminal acid challenge, increased mucus gel thickness, and elevated pHi during acid challenge.

分子量

767.89

Formula

C37H49N7O9S
CAS 号

5534-95-2
中文名称

五肽胃泌素；五肽胃必素；五肽促胃液素
运输条件

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

Protect from light

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

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (protect from light)
溶解性数据
In Vitro:;

DMSO : ≥ 34 mg/mL (44.28 mM)

H2O : 1 mg/mL (1.30 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3023 mL 6.5113 mL 13.0227 mL
5 mM 0.2605 mL 1.3023 mL 2.6045 mL
10 mM 0.1302 mL 0.6511 mL 1.3023 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 (protect from light)。-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: ≥ 2.08 mg/mL (2.71 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.71 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 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% corn oil

    Solubility: ≥ 2.08 mg/mL (2.71 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.71 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 20.8 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]. Smith AJ, et al. Characterisation of CCKB receptors on GH3 pituitary cells: receptor activation is linked to Ca2+ mobilisation. Eur J Pharmacol. 1994 Apr 15;267(2):215-23.

    [2]. Tanaka S, et al. Pentagastrin gastroprotection against acid is related to H2 receptor activation but not acid secretion. Gut. 1998 Sep;43(3):334-41.

Goserelin acetate(Synonyms: 醋酸戈舍瑞林 ICI-118630 acetate)

发表于由

Goserelin acetate;(Synonyms: 醋酸戈舍瑞林; ICI-118630 acetate) 纯度: 99.23%

Goserelin acetate (ICI-118630 acetate) 是一种促性腺激素释放激素 (GnRH/LHRH) 十肽类似物，能作为 GnRH 激动剂。Goserelin acetate 可用于乳腺癌、上皮性卵巢癌和前列腺癌的研究。

Goserelin acetateamp;;(Synonyms: 醋酸戈舍瑞林; ICI-118630 acetate)

Goserelin acetate Chemical Structure

CAS No. : 145781-92-6

规格 价格 是否有货 数量
10;mM;*;1 mL in DMSO ￥1930 In-stock
5 mg ￥910 In-stock
10 mg ￥1320 In-stock
50 mg ￥4620 In-stock
100 mg ; 询价 ;
200 mg ; 询价 ;

* Please select Quantity before adding items.

Goserelin acetate 相关产品

bull;相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • GPCR/G Protein Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Drug Repurposing Compound Library
  • Endocrinology Compound Library
  • FDA Approved amp; Pharmacopeial Drug Library
  • Anti-Breast Cancer Compound Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Targeted Diversity Library
  • Rare Diseases Drug Library
  • Peptide Library

生物活性

Goserelin acetate (ICI-118630 acetate), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin acetate can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer[1][2].

IC50 Target

GnRH[1]
体外研究
(In Vitro)

Goserelin (1 nM-1 mM; 48-72 hours) promotes EOC cell apoptosis[1].
Goserelin (100 μM; 24-72 hours) regulates the expression of human apoptosis-related genes in SKOV3-ip cells[1].
Goserelin (100 μM; 24-72 hours) promotes EOC cell apoptosis by upregulating FOXO1 through the PI3K/AKT signaling pathway[1].

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

Apoptosis Analysis[1]

Cell Line: SKOV3 cells, SKOV3-ip cells, A2780 cells (human EOC cell lines)
Concentration: 1 nM, 10 nM, 100 nM, 1 μM, 10 μM, 100 μM, 1 mM
Incubation Time: 48 hours, 72 hours
Result: Significantly increased the total apoptosis rate of SKOV3-ip, SKOV3 and A2780 cells.

Western Blot Analysis[1]

Cell Line: SKOV3 cells, SKOV3-ip cells, A2780 cells (human EOC cell lines)
Concentration: 1 nM, 10 nM, 100 nM, 1 μM, 10 μM, 100 μM, 1 mM
Incubation Time: 48 hours, 72 hours
Result: The expression of cleaved-caspase-3 and cleaved-PARP were observably increased at 100 μM.

RT-PCR[1]

Cell Line: SKOV3-ip cells
Concentration: 100 μM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: Expression of human apoptosis-related genes regulated

体内研究
(In Vivo)

Goserelin (100 µg; s.c.; daily; for 19 days) significantly increases the proportion of apoptotic cells in the subcutaneous xenograft tumors[1].

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

Animal Model: Five-week-old specific-pathogen free (SPF) female nude mice (18-20 g), subcutaneous xenograft tumor model[1]
Dosage: 100 µg/mice
Administration: Subcutaneous injection, daily, for 19 days
Result: Significantly increased the proportion of apoptotic cells in the subcutaneous xenograft tumors

Clinical Trial

分子量

1329.46

Formula

C61H88N18O16
CAS 号

145781-92-6
中文名称

醋酸戈舍瑞林
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:;

H2O : 100 mg/mL (75.22 mM; Need ultrasonic)

DMSO : ≥ 28 mg/mL (21.06 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.7522 mL 3.7609 mL 7.5219 mL
5 mM 0.1504 mL 0.7522 mL 1.5044 mL
10 mM 0.0752 mL 0.3761 mL 0.7522 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: ≥ 2.08 mg/mL (1.56 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (1.56 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (1.56 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (1.56 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 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: 2.08 mg/mL (1.56 mM); Clear solution; Need warming

    此方案可获得 2.08 mg/mL (1.56 mM) 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 20.8 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]. Ning Zhang, et al. Goserelin promotes the apoptosis of epithelial ovarian cancer cells by upregulating forkhead box O1 through the PI3K/AKT signaling pathway. Oncol Rep. 2018 Mar; 39(3): 1034–1042.

    [2]. Halle C F Moore, et al. Goserelin for ovarian protection during breast-cancer adjuvant chemotherapy. N Engl J Med. 2015 Mar 5;372(10):923-32.

ICI-192,605 品牌：FUJIFILM Wako

发表于由

ICI-192,605

品牌：FUJIFILM Wako
CAS No.：117621-64-4
储存条件：-20℃
纯度：–
产品编号

(生产商编号)

 等级 规格 运输包装 零售价(RMB) 库存情况 参考值

095-04231

 for Biochemistry 10 mg –

ICI-192,605 品牌：FUJIFILM Wako

 – –


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