AMG 837 calcium hydrate

Name: AMG 837 calcium hydrate
Brand: MedChemExpress
SKU: HY-13967B
Rating: 4.5 (1 reviews)

Cat. No.: HY-13967B Purity: 98.45%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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. AMG 837 (calcium hydrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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

AMG 837 calcium hydrate Chemical Structure

CAS No. : 1259389-38-2

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 110	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 110	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 620	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 990	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of AMG 837 calcium hydrate:

AMG 837 hemicalcium Get quote
AMG 837 Get quote
AMG 837 sodium salt Get quote

1 Publications Citing Use of MCE AMG 837 calcium hydrate

•Biomed Pharmacother. 2023 May.

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Biological Activity
Purity & Documentation
References
Customer Review

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]. AMG 837 (calcium hydrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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].

MedChemExpress (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].

MedChemExpress (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

C₂₆H₂₁F₃O₃.1/2Ca.H₂O

CAS No.

1259389-38-2

Appearance

Solid

Color

White to off-white

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.[Ca2+].O

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.45%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (248 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

References

[1]. Daniel CHL, 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. [Content Brief]

[2]. Houze JB, et, al. AMG 837: a potent, orally bioavailable GPR40 agonist. Bioorg Med Chem Lett. 2012 Jan 15; 22(2): 1267-70. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1956 mL	10.9782 mL	21.9563 mL	54.8908 mL
	5 mM	0.4391 mL	2.1956 mL	4.3913 mL	10.9782 mL
	10 mM	0.2196 mL	1.0978 mL	2.1956 mL	5.4891 mL
	15 mM	0.1464 mL	0.7319 mL	1.4638 mL	3.6594 mL
	20 mM	0.1098 mL	0.5489 mL	1.0978 mL	2.7445 mL
	25 mM	0.0878 mL	0.4391 mL	0.8783 mL	2.1956 mL
	30 mM	0.0732 mL	0.3659 mL	0.7319 mL	1.8297 mL
	40 mM	0.0549 mL	0.2745 mL	0.5489 mL	1.3723 mL
	50 mM	0.0439 mL	0.2196 mL	0.4391 mL	1.0978 mL
	60 mM	0.0366 mL	0.1830 mL	0.3659 mL	0.9148 mL
	80 mM	0.0274 mL	0.1372 mL	0.2745 mL	0.6861 mL