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  3. AMG 837 calcium hydrate

AMG 837 calcium hydrate 

Cat. No.: HY-13967B Purity: 97.23%
Handling Instructions

AMG 837 calcium hydrate is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 calcium hydrate inhibits specific [3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 calcium hydrate could enhance insulin secretion and lower glucose levels in rodents.

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

AMG 837 calcium hydrate Chemical Structure

AMG 837 calcium hydrate Chemical Structure

CAS No. : 1259389-38-2

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Solution
10 mM * 1 mL in DMSO USD 145 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 145 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 204 In-stock
Estimated Time of Arrival: December 31
50 mg USD 780 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

AMG 837 calcium hydrate is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 calcium hydrate inhibits specific [3H]AMG 837 binding at the human FFA1 receptor with a pIC50 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 EC50 of 142±20 nM on islets isolated from mice[1].
AMG 837 stimulates Ca2+ flux with the EC50s 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 Cmax 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.
Molecular Weight

455.45

Formula

C₂₆H₂₂F₃O₄-

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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 provided by MCE.
References
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Product Name:
AMG 837 calcium hydrate
Cat. No.:
HY-13967B
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