[CAS NO. 1259389-38-2] AMG837calciumhydrate

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PRODUCTS SPECIFICATIONS [1259389-38-2]

Catalog

HY-13967B

Brand

MCE

CAS

1259389-38-2

DESCRIPTION [1259389-38-2]

Overview

MDL	MFCD28167803
Molecular Weight	455.45
Molecular Formula	C26H21F3O3.1/2Ca.H2O
SMILES	[O-]C(C[C@H](C#CC)C1=CC=C(C=C1)OCC2=CC=CC(C3=CC=C(C(F)(F)F)C=C3)=C2)=O.[0.5Ca2+].O

For research use only. We do not sell to patients.

Summary

AMG 837 calcium hydrate is a potent, orally bioavailable and partial agonist of GPR40/FFA1 . AMG 837 calcium hydrate inhibits specific [ ³ H]AMG 837 binding at the human FFA1 receptor with a pIC ₅₀ of 8.13. AMG 837 calcium hydrate could enhance insulin secretion and lower glucose levels in rodents ^[1] ^[2] ^[3] .

IC50 & Target

pIC50: 8.13 (FFA1) ^[3]

In Vitro

AMG 837 (1 nM-10 μM) stimulates insulin secretion in a glucose-dependent manner with an EC ₅₀ of 142±20 nM on islets isolated from mice ^[1] .
AMG 837 stimulates Ca ²⁺ flux with the EC ₅₀ s of 13.5, 22.6 and 31.7 nM for human, mouse and rat receptors in CHO cells, respectively ^[1] .

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

In Vivo

AMG 837 (0.03-0.3 mg/kg; p.o. once daily for 21 days) reduces glucose levels and increases insulin levels following glucose challenge in vivo ^[1] .
AMG 837 (0.03-0.3 mg/kg; a single p.o.) improves glucose tolerance and enhances insulin secretion in Sprague-Dawley rats ^[1] .
AMG 837 (0.5 mg/kg; p.o.) displays excellent oral bioavailability (F = 84%) and a total plasma C _max of 1.4 µM ^[1] .

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

Animal Model:	8-week old Zucker Fatty Rats ^[1]
Dosage:	0.03, 0.1, 0.3 mg/kg
Administration:	Oral gavage once daily for 21 days
Result:	Decreased glucose AUC values during the glucose tolerance test (GTT) to 7%, 15%, and 25% at 0.03, 0.1 and 0.3 mg/kg, respectively. Increased insulin levels in the mid- and high-dose groups. Not affected body weights during the 21-day treatment.

Animal Model:	8-week old Sprague-Dawley rats ^[1]
Dosage:	0.03, 0.1, 0.3 mg/kg
Administration:	A single p.o. administration
Result:	Reduced the post-prandial glucose with the half-maximal dose of 0.05 mg/kg.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 42 mg/mL ( 92.22 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1956 mL	10.9782 mL	21.9563 mL
5 mM	0.4391 mL	2.1956 mL	4.3913 mL
10 mM	0.2196 mL	1.0978 mL	2.1956 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: 2.5 mg/mL (5.49 mM); Suspended solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

* All of the co-solvents are available by MCE.