[CAS NO. 834903-43-4] CID16020046

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PRODUCTS SPECIFICATIONS [834903-43-4]

Catalog

HY-16697

Brand

MCE

CAS

834903-43-4

DESCRIPTION [834903-43-4]

Overview

MDL	MFCD06196075
Molecular Weight	425.44
Molecular Formula	C25H19N3O4
SMILES	O=C(O)C1=CC=C(N(C2C3=CC=CC(O)=C3)C(C4=C2C(C5=CC=C(C)C=C5)=NN4)=O)C=C1

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

1 Publications Citing Use of MCE

[1]Autophagy. 2021 Nov;17(11):3592-3606.

Summary

CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC ₅₀ of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca ²⁺ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function ^[1] .

In Vitro

CID 16020046 has weak activities close for inhibition of the acetylcholinesterase (pIC ₅₀ =4.4), antagonism of the m-opioid receptor (pIC ₅₀ =4.6), and blockade of KCNH2, the hERG channel (pIC ₅₀ =4.6) 6 in human embryonic kidney (HEK)-G protein–coupled receptor 55 (GPR55) cells ^[1] .
CID 16020046 (2.5 μM; for ≥25 minutes) significantly inhibits the lysophosphatidylinositol (LPI; 2.5 μM) induced ERK1/2 phosphorylation. CID 16020046 alone fails to induce intracellular Ca ²⁺ release in HEK-GPR55, HEKCB1 cells and shows no ERK1/2 phosphorylation ^[1] .
Pretreatment with CID16020046 (0.01, 0.1, 1, 10 μM) leads to a concentration-dependent decrease in GPR55-mediated NFAT activation, NF-kB activation, and SRE induction in response to 1 μM LPI or GSK319197A in HEKGPR55 and HEK-CB1 cells ^[1] .
CID16020046 (2.5 μM) antagonizes GPR55-mediated activation and nuclear translocation of transcription factors but has no effect on CB1-mediated CREB activation ^[1] .
Pretreatment CID16020046 (1 μM) abolished the LPI-induced stimulation of wound healing in HMVEC-Ls ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line:	HEK-CB1 and HEK-CB2 cells ^[1]
Concentration:	2.5 μM
Incubation Time:	For ≥25 minutes
Result:	Significantly inhibited the LPI (2.5 μM) induced ERK1/2 phosphorylation. Treatment alone showed no ERK1/2 phosphorylation and did not alter WIN55,212-2 (2.5 μM) induced ERK1/2 phosphorylation in HEK-CB1 and HEK-CB2 cells.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 235.05 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3505 mL	11.7525 mL	23.5051 mL
5 mM	0.4701 mL	2.3505 mL	4.7010 mL
10 mM	0.2351 mL	1.1753 mL	2.3505 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Kargl J, et al. A selective antagonist reveals a potential role of G protein-coupled receptor 55 in platelet and endothelial cell function. J Pharmacol Exp Ther. 2013 Jul;346(1):54-66.

Synonyms

Benzoic acid, 4-[4,6-dihydro-4-(3-hydroxyphenyl)-3-(4-methylphenyl)-6-oxopyrrolo[3,4-c]pyrazol-5(1H)-yl]-

4-[4,6-Dihydro-4-(3-hydroxyphenyl)-3-(4-methylphenyl)-6-oxopyrrolo[3,4-c]pyrazol-5(1H)-yl]benzoic acid

CID 16020046