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533469 GPR120 Agonist IV, cpdA - CAS 1599477-75-4 - Calbiochem

GPR120 Agonist CpdA

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: 2-(3-(2-Chloro-5-(trifluoromethoxy)phenyl)-3-azaspiro[5.5]undecan-9-yl)acetic acid

Primary Target: GPR120
533469
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Aperçu

Replacement Information

Tableau de caractéristiques principal

CAS #Empirical Formula
1599477-75-4C₁₉H₂₃ClF₃NO₃

Products

RéférenceConditionnement Qté
5334690001 Flacon en verre 10 mg
Description
OverviewA cell-permeable, orally active, non-toxic, azaspiroundecanyl acetic acid based compound that acts as a highly potent, selective and reversible activator of GPR120 in murine and human cells (EC50 = 350 nM for β-arrestin 2 recruitment). Induces concentration-dependent increase in inositol-1,4,5-triphosphate (IP3) production in GRP120 expressing cells. Exhibits about 50-fold higher sensitivity for GRP120 than docosahexaenoic acid, however, it displays very poor affinity towards GRP40. Effectively reduces hepatic steatosis and improves glucose tolerance, hyperinsulinemia, and insulin sensitivity in obese mice fed high fat diet. Strongly inhibits LPS-induced phosphorylation of TAK1, IKKβ & JNK and reduces IκB degradation in macrophages.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Catalogue Number533469
Brand Family Calbiochem®
Synonyms2-(3-(2-Chloro-5-(trifluoromethoxy)phenyl)-3-azaspiro[5.5]undecan-9-yl)acetic acid
References
ReferencesOh, D.Y., et al. 2014. Nat. Med. 8, 942.
Product Information
CAS number1599477-75-4
FormOff-white solid
Hill FormulaC₁₉H₂₃ClF₃NO₃
Chemical formulaC₁₉H₂₃ClF₃NO₃
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary TargetGPR120
Purity≥97% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Référence GTIN
5334690001 04055977286953

Documentation

GPR120 Agonist IV, cpdA - CAS 1599477-75-4 - Calbiochem FDS

Titre

Fiche de données de sécurité des matériaux (FDS) 

Références bibliographiques

Aperçu de la référence bibliographique
Oh, D.Y., et al. 2014. Nat. Med. 8, 942.
Fiche technique

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision23-July-2016 JSW
Synonyms2-(3-(2-Chloro-5-(trifluoromethoxy)phenyl)-3-azaspiro[5.5]undecan-9-yl)acetic acid
DescriptionA cell-permeable azaspiroundecanyl acetic acid compound that acts as a selective Gpr120 (FFAR4) agonist toward both human and murine species (EC50 = 60 nM/IP3 production and 350 nM/β-Arrestin-2 recruitment using cells expressing human or murine Gpr120), while being ineffective toward Gpr40 and is about 100-fold more effective than docosahexaenoic acid/DHA in stimulating serum response element/SRE promoter-mediated reporter transcription in mGPR120-expressing HEK 293. Selectively suppresses (10 µM) chemotaxis toward adipocyte-conditioned medium and LPS-induced inflammatory responses in primary macrophages derived from wt, but not Gpr120-knockout, mice in vitro, including IκB degradation as well as phosphorylations of Tak1, Ikk-β, and JNK, and is efficacious in improving glucose tolerance & insulin sensitivity in vivo among wt, but not Gpr120-knockout, mice on high-fat diet (HFD) when supplemented (30 mg/kg) in the diet for the last 5 wks of a 20-wk HFD period without affecting animal body weight, resulting in decreased hyperinsulinemia, hepatic steatosis, adipose tissue macrophage (ATM) infiltration and inflammation. Unlike the Gpr40/Gpr120 dual agonist DHA, this compound does not stimulate Gpr40-mediated insulin secretion from MIN6 β cell line or ehances Glucose-stimulated insulin secretion (GSIS) from β cells in cultured islets from wt or Gpr120-knockout mice.
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1599477-75-4
Chemical formulaC₁₉H₂₃ClF₃NO₃
Purity≥97% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesOh, D.Y., et al. 2014. Nat. Med. 8, 942.