ChemicalBook > CAS DataBase List > GW-1100

GW-1100

Product Name
GW-1100
CAS No.
306974-70-9
Chemical Name
GW-1100
Synonyms
GW-1100;GW1100;GW1100;GPR40 Antagonist, GW1100 - CAS 306974-70-9 - Calbiochem;1-(4-Ethoxycarbonylphenyl)-2-(4-fluorobenzylthio)-5-(2-ethoxy-5-pyrimidinylmethyl)-4-pyrimidinone;Benzoic acid, 4-[5-[(2-ethoxy-5-pyrimidinyl)methyl]-2-[[(4-fluorophenyl)methyl]thio]-4-oxo-1(4H)-pyrimidinyl]-, ethyl ester
CBNumber
CB01872299
Molecular Formula
C27H25FN4O4S
Formula Weight
520.58
MOL File
306974-70-9.mol
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GW-1100 Property

Melting point:
208-210℃
Boiling point:
690.2±65.0 °C(Predicted)
Density 
1.29±0.1 g/cm3(Predicted)
storage temp. 
+2C to +8C
solubility 
Soluble in DMSO (up to 2 mg/ml) or in DMF (up to 5 mg/ml).
form 
White powder
pka
1.20±0.22(Predicted)
color 
White
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or DMF may be stored at -20° for up to 3 months. Dilutions into aqueous media are not stable and should be used within one working day.
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
371830
Product name
GPR40 Antagonist, GW1100 - CAS 306974-70-9 - Calbiochem<br />The GPR40 Antagonist, GW1100, also referenced under CAS 306974-70-9, controls the biological activity of GPR40. This small molecule/inhibitor is primarily used for Biochemicals applications.
Packaging
10mg
Price
$308
Updated
2024/03/01
Cayman Chemical
Product number
10008908
Product name
GW 1100
Purity
≥95%
Packaging
5mg
Price
$73
Updated
2024/03/01
Cayman Chemical
Product number
10008908
Product name
GW 1100
Purity
≥95%
Packaging
10mg
Price
$138
Updated
2024/03/01
Cayman Chemical
Product number
10008908
Product name
GW 1100
Purity
≥95%
Packaging
25mg
Price
$217
Updated
2024/03/01
Cayman Chemical
Product number
10008908
Product name
GW 1100
Purity
≥95%
Packaging
50mg
Price
$396
Updated
2024/03/01
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GW-1100 Chemical Properties,Usage,Production

Description

GW1100 (306974-70-9) is a selective antagonist of GPR40. GW1100 inhibits GRP40-mediated Ca2+?increases stimulated by GW9508 (Cat.# 10-1108) or linoleic acid (pIC50?= 5.99 for either agonist).1?The effects of GPR40 activation on insulin secretion in cells are also blocked by the addition of GW1100. GW1100 does not influence calcium mobilization mediated by GPR120.

Uses

GW 1100 is a selective G protein-coupled receptor GPR40 antagonist. GW 1100 has been shown to reverse the effects GPR40 agonists which induce glucose-stimulated insulin secretion.

Biological Activity

GW-1100 is a selective GPR40 antagonist with pIC50 of 6.9.

in vitro

GW-1100 (GW1100) dose dependently inhibits GPR40-mediated Ca 2+ elevations stimulated by GW9508 and linoleic acid (pIC 50 values of 5.99±0.03 and 5.99±0.06, respectively). GW-1100 at a concentration of 1 μM produces a significant rightward shift in the concentration-response curve to GW9508 (pEC 50 =7.17±0.08 in the absence and pEC 50 =6.79±0.09 in the presence of 1 μM GW-1100; P<0.05; n=3). At concentrations of GW-1100 of 3 μM and higher a significant decrease in the maximal response is observed with a continuing rightward shift in the pEC 50 response. GW-1100 (GW1100) reduces FFAR1 ligand-induced intracellular calcium in CHO-K1/bFFAR1 cells and neutrophils. CHO-K1/bFFAR1 cells are incubated for 15 min with 10 μM GW1100 or vehicle (0.1% DMSO) and then stimulated with vehicle, oleic acid, linoleic acid or GW9508. GW-1100 significantly reduces the increase in intracellular calcium induced by 300 μM oleic acid (AUC (60-150 s) , p<0.05), 100 μM linoleic acid (AUC (60-150 s) , p<0.05) and 10 μM GW9508 (AUC (60-150 s) , p<0.05).

in vivo

The intracerebroventricular injection of DHA (50 μg) and GW9508 (1.0 μg), a GPR40-selective agonist, significantly reduces mechanical allodynia and thermal hyperalgesia at day 7, but not at day 1, after CFA injection. These effects are inhibited by intracerebroventricular pretreatment with GW-1100 (10 μg), a GPR40 antagonist.

References

1) Brisco?et al. (2006),?Pharmacological regulation of insulin secretion in MIN6 cells through fatty acid receptor GPR40: identification of agonist and antagonist molecules; Br. J. Pharmacol.,?148?619 2) Nagatake?et al. (2018),?The 17,18-Epoxytetraenoic acid-G protein-coupled receptor 40 axis ameliorates contact hypersensitivity by inhibiting neutrophil mobility in mice and cynomolgus macaques; J. Allergy Clin. Immunol.,?142?470 [Focus Biomolecules Citation]

GW-1100 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from GW-1100 manufacturers

Career Henan Chemical Co
Product
GW-1100 306974-70-9
Price
US $7.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
100KG
Release date
2018-08-20

306974-70-9, GW-1100Related Search:


  • Benzoic acid, 4-[5-[(2-ethoxy-5-pyrimidinyl)methyl]-2-[[(4-fluorophenyl)methyl]thio]-4-oxo-1(4H)-pyrimidinyl]-, ethyl ester
  • GW-1100
  • GPR40 Antagonist, GW1100 - CAS 306974-70-9 - Calbiochem
  • GW1100;GW1100
  • 1-(4-Ethoxycarbonylphenyl)-2-(4-fluorobenzylthio)-5-(2-ethoxy-5-pyrimidinylmethyl)-4-pyrimidinone
  • 306974-70-9
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Aromatics
  • Heterocycles