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| 10mg |
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| 25mg |
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Purity: ≥98%
AMG 837 calcium hydrate is a novel, orally bioavailable and potent GPR40 agonist with EC50 of 13 nM and with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.It has been suggested that type 2 diabetes can be treated with GPR40 (FFA1) antagonists. GTPγS binding, inositol phosphate accumulation, and Ca(2+) flux assays were used to characterize the activity of AMG 837 on GPR40. Using isolated primary mouse islets, the effect of AMG 837 on insulin release was evaluated. In both vitro and in vivo glucose-stimulated insulin secretion, AMG 837 was a strong partial agonist on the GPR40 receptor in the calcium flux assay. In glucose tolerance tests, both normal and Zucker fatty rats administered acutely to AMG 837 showed reduced glucose excursions and increased glucose-stimulated insulin secretion. After daily administration of AMG 837 for 21 days, the Zucker fatty rats' improvement in glucose excursions continued. AMG 837 was shown in preclinical research to be a strong GPR40 partial agonist that decreased postprandial glucose levels. The possible benefit of AMG 837 for the management of type 2 diabetes is supported by these studies.
| Targets |
FFA1 ( pIC50 = 8.13 )
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|---|---|
| ln Vitro |
AMG 837 (1 nM–10 μM) stimulates insulin secretion in a glucose-dependent manner with an EC50 of 142±20 nM on islets isolated from mice[1].
AMG 837 increases Ca2+ flux in CHO cells with EC50 values of 13.5, 22.6, and 31.7 nM for rat, mouse, and human receptors, respectively[1]. |
| ln Vivo |
AMG 837 (0.03-0.3 mg/kg; p.o. once daily for 21 days) lowers blood glucose and raises insulin levels after a glucose challenge in vivo[1].
AMG 837 (0.03-0.3 mg/kg; one oral dose) increases insulin secretion and glucose tolerance in Sprague-Dawley rats[1]. AMG 837 (0.5 mg/kg; p.o.) exhibits a total plasma Cmax of 1.4 µM and good oral bioavailability (F = 84%)[1]. |
| Animal Protocol |
8-week old Zucker Fatty Rats
0.03, 0.1, 0.3 mg/kg Oral gavage once daily for 21 days |
| References |
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| Molecular Formula |
C52H42CAF6O7
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|---|---|
| Molecular Weight |
932.954115390778
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| Exact Mass |
932.25
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| Elemental Analysis |
C, 66.94; H, 4.54; Ca, 4.30; F, 12.22; O, 12.00
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| CAS # |
1259389-38-2
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| Related CAS # |
AMG 837 hemicalcium; 1291087-14-3; AMG 837; 865231-46-5; AMG 837 sodium salt; 865231-45-4
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| Appearance |
Solid powder
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| SMILES |
CC#C[C@@H](CC(=O)[O-])C1=CC=C(C=C1)OCC2=CC(=CC=C2)C3=CC=C(C=C3)C(F)(F)F.CC#C[C@@H](CC(=O)[O-])C1=CC=C(C=C1)OCC2=CC(=CC=C2)C3=CC=C(C=C3)C(F)(F)F.O.[Ca+2]
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| InChi Key |
QDINKBCSIAWNMP-XYDYARRRSA-L
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| InChi Code |
InChI=1S/2C26H21F3O3.Ca.H2O/c2*1-2-4-21(16-25(30)31)20-9-13-24(14-10-20)32-17-18-5-3-6-22(15-18)19-7-11-23(12-8-19)26(27,28)29;;/h2*3,5-15,21H,16-17H2,1H3,(H,30,31);;1H2/q;;+2;/p-2/t2*21-;;/m00../s1
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| Chemical Name |
calcium;(3S)-3-[4-[[3-[4-(trifluoromethyl)phenyl]phenyl]methoxy]phenyl]hex-4-ynoate;hydrate
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| Synonyms |
AMG 837; AMG837; AMG-837; AMG 837 hemicalcium hydrate; AMG 837 hemicalcium salt
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 42 mg/mL (~92.2 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.49 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.49 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0719 mL | 5.3593 mL | 10.7187 mL | |
| 5 mM | 0.2144 mL | 1.0719 mL | 2.1437 mL | |
| 10 mM | 0.1072 mL | 0.5359 mL | 1.0719 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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