CID-16020046


Catalog No. Size PriceQuantity
M7252-2 2mg solid $95
M7252-10 10mg solid $285

Description

CID-16020046 is a selective GPR55 LPI receptor antagonist with IC50 of 015 M

Product information

CAS Number: 834903-43-4

Molecular Weight: 425.44

Formula: C25H19N3O4

Synonym:

C390-0219

Chemical Name: 4-[4-(3-hydroxyphenyl)-3-(4-methylphenyl)-6-oxo-1,4-dihydropyrrolo[3,4-d]pyrazol-5-yl]benzoic acid

Smiles: CC1C=CC(=CC=1)C1=NNC2=C1C(C1=CC(O)=CC=C1)N(C1C=CC(=CC=1)C(O)=O)C2=O

InChiKey: VGUQVYZXABOXCX-UHFFFAOYSA-N

InChi: InChI=1S/C25H19N3O4/c1-14-5-7-15(8-6-14)21-20-22(27-26-21)24(30)28(18-11-9-16(10-12-18)25(31)32)23(20)17-3-2-4-19(29)13-17/h2-13,23,29H,1H3,(H,26,27)(H,31,32)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 85 mg/mL(199.79 mM). Water: Insoluble.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

In yeast cells expressing human GPR55, CID16020046 antagonized agonist-induced receptor activation. In human embryonic kidney (HEK293) cells stably expressing human GPR55, the compound behaved as an antagonist on LPI-mediated Ca2+ release and extracellular signal-regulated kinases activation, but not in HEK293 cells expressing cannabinoid receptor 1 or 2 (CB1 or CB2). CID16020046 concentration dependently inhibited lysophosphatidylinositol (LPI)-induced activation of nuclear factor of activated T-cells (NFAT), nuclear factor κ of activated B cells (NF-κB) and serum response element, translocation of NFAT and NF-κB, and GPR55 internalization[2].

In Vivo:

CID16020046 improves inflammation in models of intestinal inflammation and reduces proinflammatory cytokines. CID16020046 does not change the locomotor and anxiety behavior of healthy mice[1].

References:

  1. Angela Stančić, et al. Neurogastroenterol Motil. 2015, 27(10): 1432-1445.
  2. Kargl J, et al. J Pharmacol Exp Ther. 2013, 346(1):54-66.

Products are for research use only. Not for human use.

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