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AMG 837 calcium hydrate

Catalog No. TQ0020 CAS 1259389-38-2

AMG 837 calcium hydrate is a potent GPR40 agonist with an EC50 of 13 nM. AMG 837 calcium hydrate also shows highly selective over GPR41, GPR43, and GPR120 (EC50 < 10,000 nM).

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AMG 837 calcium hydrate Chemical Structure

AMG 837 calcium hydrate, CAS 1259389-38-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 36.00
2 mg	In stock	$ 51.00
5 mg	In stock	$ 80.00
10 mg	In stock	$ 122.00
25 mg	In stock	$ 257.00
50 mg	In stock	$ 513.00
100 mg	In stock	$ 729.00
200 mg	In stock	$ 995.00
1 mL * 10 mM (in DMSO)	In stock	$ 89.00

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Purity: 98.07%

Biological Description

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Description	AMG 837 calcium hydrate is a potent GPR40 agonist with an EC50 of 13 nM. AMG 837 calcium hydrate also shows highly selective over GPR41, GPR43, and GPR120 (EC50 > 10,000 nM).
Targets&IC50	FFA1/GPR40:13 nM (EC50)
In vitro	GPR40 agonist AMG 837 displayed the expected two-fold increase in potency on GPR4 (EC50: 13 nM) compared to the racemic compound and its activity crossed over to the rat and mouse forms of GPR40 (EC50s: 23/13 nM). AMG 837 was a partial agonist on GPR40 with maximal activity 85% of that shown by DHA. An external panel of 64 receptors also revealed no significant activity with the exception of weak inhibition (IC50: 3 μM) on the α2-adrenergic receptor [1].
In vivo	In rats, AMG 837 increases insulin release when glucose levels are elevated [2].

Molecular Weight	950.97
Formula	C52H44CaF6O8
CAS No.	1259389-38-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 40 mg/mL (87.83 mM)

References and Literature

1. Houze JB, et al. AMG 837: a potent, orally bioavailable GPR40 agonist. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1267-70. 2. Lin DC, et al. AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents. PLoS One. 2011;6(11):e27270. 3. Daniel CHL, et, al. Identification and pharmacological characterization of multiple allosteric binding sites on the free fatty acid 1 receptor. Mol Pharmacol. 2012 Nov;82(5):843-59.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library GPCR Compound Library Orally Active Compound Library Endocrinology-Hormone Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

AMG 837 calcium hydrate 1259389-38-2 Endocrinology/Hormones GPCR/G Protein GPR AMG 837 calcium FFAR AMG 837 calcium Hydrate insulin FFA1 Inhibitor Free Fatty Acid Receptor inhibit glucose GPR40 inhibitor

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