AMY-101 acetate (Cp40 acetate), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 acetate (Cp40 acetate) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation[1][2].
IC50 Target
KD: 0.5 nM (C3)[1].
体内研究 (In Vivo)
AMY-101 can improve the periodontal condition of NHPs with natural chronic periodontitis[1]. AMY-101 can induce a long-lasting anti-inflammatory effect[1]. AMY-101 (4 mg/kg bodyweight, subcutaneous injection. once per 24 hr for a total of 28 days) causes a significant and long-lasting reduction in PPD, an index that measures tissue destruction[1]. AMY-101 (Cp40, 1 mg/kg, sc, injection every 12 h, daily, 7 or 14 days) attenuates fibrosis and infiltration of inflammatory cells in UUO-induced renal fibrosis[3].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Fifteen adult male cynomolgus monkeys (Macaca fascicularis) (7-15 years old; 5.0-7.6 kg body weight)[1].
Dosage:
0.1 mg/site; 50 μL of 2 mg/mL solution.
Administration:
Injected locally. (Either three times per week or once a week for 6 weeks followed by a 6-week follow-up period without treatment.)
Result:
Does not cause irritation in healthy gingiva.
Animal Model:
UUO and sham-operated mice[3].
Dosage:
1 mg/kg.
Administration:
Subcutaneous injection every 12 h, daily, 7 or 14 days.
Result:
1 mg/kg Cp40 had much less severe interstitial fibrosis than control peptide-injected mice.
[1]. Kajikawa T, et al. Safety and Efficacy of the Complement Inhibitor AMY-101 in a Natural Model of Periodontitis in Non-human Primates. Mol Ther Methods Clin Dev. 2017 Aug 18;6:207-215.
[2]. Mastaglio S, et al. The first case of COVID-19 treated with the complement C3 inhibitor AMY-101. Clin Immunol. 2020 Apr 29:108450.
[3]. 1 mg/kg Cp40 had much less severe interstitial fibrosis than control peptide-injected mice.
AMY-101 TFA (Cp40 TFA), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 (Cp40) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation[1][2].
IC50 Target
KD: 0.5 nM (C3)[1].
体内研究 (In Vivo)
AMY-101 can improve the periodontal condition of NHPs with natural chronic periodontitis[1]. AMY-101 can induce a long-lasting anti-inflammatory effect[1]. AMY-101 (4 mg/kg bodyweight, subcutaneous injection. once per 24 hr for a total of 28 days) causes a significant and long-lasting reduction in PPD, an index that measures tissue destruction[1]. AMY-101 (Cp40, 1 mg/kg, sc, injection every 12 h, daily, 7 or 14 days) attenuates fibrosis and infiltration of inflammatory cells in UUO-induced renal fibrosis[3].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Fifteen adult male cynomolgus monkeys (Macaca fascicularis) (7-15 years old; 5.0-7.6 kg body weight)[1].
Dosage:
0.1 mg/site; 50 μL of 2 mg/mL solution.
Administration:
Injected locally. (Either three times per week or once a week for 6 weeks followed by a 6-week follow-up period without treatment.)
Result:
Does not cause irritation in healthy gingiva.
Animal Model:
UUO and sham-operated mice[3].
Dosage:
1 mg/kg.
Administration:
Subcutaneous injection every 12 h, daily, 7 or 14 days.
Result:
1 mg/kg Cp40 had much less severe interstitial fibrosis than control peptide-injected mice.
Room temperature in continental US; may vary elsewhere.
储存方式
Sealed storage, away from moisture and light
Powder
-80deg;C
2 years
-20deg;C
1 year
*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro:;
H2O : 100 mg/mL (Need ultrasonic)
DMSO : 100 mg/mL (Need ultrasonic)
参考文献
[1]. Kajikawa T, et al. Safety and Efficacy of the Complement Inhibitor AMY-101 in a Natural Model of Periodontitis in Non-human Primates. Mol Ther Methods Clin Dev. 2017 Aug 18;6:207-215.
[2]. Mastaglio S, et al. The first case of COVID-19 treated with the complement C3 inhibitor AMY-101. Clin Immunol. 2020 Apr 29:108450.
[3]. Yanyan Liu, et al. Complement C3 Produced by Macrophages Promotes Renal Fibrosis via IL-17A Secretion. Front Immunol. 2018 Oct 22;9:2385.
AMY-101 (Cp40), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 (Cp40) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation[1][2].
IC50 Target
KD: 0.5 nM (C3)[1].
体内研究 (In Vivo)
AMY-101 can improve the periodontal condition of NHPs with natural chronic periodontitis[1]. AMY-101 can induce a long-lasting anti-inflammatory effect[1]. AMY-101 (4 mg/kg bodyweight, subcutaneous injection. once per 24 hr for a total of 28 days) causes a significant and long-lasting reduction in PPD, an index that measures tissue destruction[1]. AMY-101 (Cp40, 1 mg/kg, sc, injection every 12 h, daily, 7 or 14 days) attenuates fibrosis and infiltration of inflammatory cells in UUO-induced renal fibrosis[3].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Fifteen adult male cynomolgus monkeys (Macaca fascicularis) (7-15 years old; 5.0-7.6 kg body weight)[1].
Dosage:
0.1 mg/site; 50 μL of 2 mg/mL solution.
Administration:
Injected locally. (Either three times per week or once a week for 6 weeks followed by a 6-week follow-up period without treatment.)
Result:
Does not cause irritation in healthy gingiva.
Animal Model:
UUO and sham-operated mice[3].
Dosage:
1 mg/kg.
Administration:
Subcutaneous injection every 12 h, daily, 7 or 14 days.
Result:
1 mg/kg Cp40 had much less severe interstitial fibrosis than control peptide-injected mice.
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.
Solvent Solubility
In Vitro:;
H2O
Peptide Solubility and Storage Guidelines:
1.;;Calculate the length of the peptide.
2.;;Calculate the overall charge of the entire peptide according to the following table:
;
Contents
Assign value
Acidic amino acid
Asp (D), Glu (E), and the C-terminal -COOH.
-1
Basic amino acid
Arg (R), Lys (K), His (H), and the N-terminal -NH2
+1
Neutral amino acid
Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q)
0
3.;;Recommended solution:
Overall charge of peptide
Details
Negative (lt;0)
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, add NH4OH (lt;50 μL). 3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (gt;0)
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0)
1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献
[1]. Kajikawa T, et al. Safety and Efficacy of the Complement Inhibitor AMY-101 in a Natural Model of Periodontitis in Non-human Primates. Mol Ther Methods Clin Dev. 2017 Aug 18;6:207-215.
[2]. Mastaglio S, et al. The first case of COVID-19 treated with the complement C3 inhibitor AMY-101. Clin Immunol. 2020 Apr 29:108450
[3]. Yanyan Liu, et al. Complement C3 Produced by Macrophages Promotes Renal Fibrosis via IL-17A Secretion. Front Immunol. 2018 Oct 22;9:2385.
β-Amyloid (31-35) is the shortest sequence of native Amyloid-β peptide that retains neurotoxic activity.
体外研究 (In Vitro)
β-Amyloid (31-35) is a functional cytotoxic domain of Aβ peptide. β-Amyloid (31-35) increases the phosphorylation of biotinylated Aβ(1-40), enhances CDK-1 activity, and also inhibits binding of Aβ to cyclin B1. β-Amyloid (31-35) is cytotoxic, and such an effect can be inhibited by olomoucine in differentiated human teratocarcinoma cell line, Ntera 2/cl-D1 (NT-2) neurons[1]. β-Amyloid Aggregation Guidelines (Following is our recommended protocol. This protocol only provides a guideline, and should be modified according to your specific needs). 1. Solid Aβ peptide was dissolved in cold hexafluoro-2-propanol (HFIP). The peptide was incubated at room temperature for at least 1h to establish monomerization and randomization of structure. 2. The HFIP was removed by evaporation, and the resulting peptide was stored as a film at -20 or -80 °C. 3. The resulting film was dissolved in anhydrous DMSO at 5 mM and then diluted into the appropriate concentration and buffer (serum- and phenol red-free culture medium) with vortexing. 4. Next, the solution was age 48h at 4-8 °C. The sample was then centrifuged at 14000g for 10 min at 4-8 °C; the soluble oligomers were in the supernatant. The supernatant was diluted 10-200-fold for experiments. Methods vary depends on the downstream applications.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
545.74
Formula
C25H47N5O6S
CAS 号
149385-65-9
Sequence
Ile-Ile-Gly-Leu-Met
Sequence Shortening
IIGLM
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 : 5 mg/mL (9.16 mM; ultrasonic and adjust pH to 7 with HCl)
[1]. Milton NG, et al. The amyloid-beta peptide binds to cyclin B1 and increases human cyclin-dependent kinase-1 activity. Neurosci Lett. 2002 Apr 5;322(2):131-3.
[2]. Misiti F, et al. Fragment 31-35 of beta-amyloid peptide induces neurodegeneration in rat cerebellar granule cells via bax gene expression and caspase-3 activation. A crucial role for the redox state of methionine-35 residue. Neurochem Int. 2006 Oct;49(5):525-32.
[3]. M Jesús Pérez de Vega, et al. Synthesis and biological properties of beta-turned Abeta(31-35) constrained analogues. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2078-82.
