Free shipping on all orders over $ 500

GSK137647A

Cat. No. M5187
GSK137647A Structure
Synonym:

GSK 137647

Size Price Availability Quantity
5mg USD 50  USD50 In stock
10mg USD 80  USD80 In stock
50mg USD 260  USD260 In stock
100mg USD 400  USD400 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

GSK137647A is a selective FFA4 agonist for human, Mouse and Rat FFA4 with pEC50 values of 6.3, 6.2 and 6.1, respectively. GSK137647A is shown to provide at least 100-fold selectivity against the panel which included 41 G-protein-coupled receptors. Under high glucose conditions (25 mM), GSK137647A produces a concentration-dependent increase in glucose stimulated insulin secretion.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 305.39
Formula C16H19NO3S
CAS Number 349085-82-1
Purity >98%
Solubility DMSO 30 mg/mL
Storage at -20°C
References

[1] Sparks SM, et al. Bioorg Med Chem Lett. Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).

Related GPR Products
WAY-388798

WAY-388798 is a agonist of free fatty acid receptor 1 (GPR40)

NE 52-QQ57

NE 52-QQ57 is an orally available GPR4 antagonist with an IC50 of 70 nM. NE 52-QQ57 significantly inhibited the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2).

GPR81 agonist 1

GPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC50 values of 58 nM and 50 nM for human and mouse GPR81, respectively.

MCH TFA (human, mouse, rat)

MCH TFA (human, mouse, rat) is a potent peptide agonist of MCH-R and exhibits binding IC50 values of 0.3nM and 1.5 nM for MCH1R and MCH2R, respectively.

AF64394

AF64394 is a selective GPR3 inverse agonist with a pIC50 of 7.3.

  Catalog
Abmole Inhibitor Catalog




Keywords: GSK137647A, GSK 137647 supplier, GPR, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.