PSNCBAM-1

Cat. No.: HY-110179 Purity: 99.48%: FAQs
Data Sheet SDS COA Handling Instructions

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PSNCBAM-1 is a selective CB1 receptor allosteric antagonist with an EC₅₀ of 0.1 μM. PSNCBAM-1 can be used in the researches of obesity.

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

PSNCBAM-1 Chemical Structure

CAS No. : 877202-74-9

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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CB1 CB2

Biological Activity
Purity & Documentation
References
Customer Review

Description

PSNCBAM-1 is a selective CB1 receptor allosteric antagonist with an EC₅₀ of 0.1 μM. PSNCBAM-1 can be used in the researches of obesity^[1].

IC₅₀ & Target

hCB1-R

0.1 μM (EC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	> 10 μM Compound: 2; PSNCBAM-1	Antagonist activity at human CB2 receptor expressed in CHO cells co-expressing Galpha16 assessed as inhibition of EC80 CP55,940-induced calcium mobilization preincubated for 15 mins followed by CP55,490 addition measured at 1 sec interval for 90 secs by c Antagonist activity at human CB2 receptor expressed in CHO cells co-expressing Galpha16 assessed as inhibition of EC80 CP55,940-induced calcium mobilization preincubated for 15 mins followed by CP55,490 addition measured at 1 sec interval for 90 secs by c	[PMID: 31596583]
CHO-K1	EC₅₀	3.84 nM Compound: 2; PSNCBAM-1	Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as inhibition of CP55,940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55,940 addition measured for 90 mins by PathHunter assay Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as inhibition of CP55,940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55,940 addition measured for 90 mins by PathHunter assay	[PMID: 26529344]
CHO-K1	EC₅₀	70.8 nM Compound: 2; PSNCBAM-1	Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as effect on CP55,940-induced inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by CP55,940 addition measured for 30 mins by HitHunte Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as effect on CP55,940-induced inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by CP55,940 addition measured for 30 mins by HitHunte	[PMID: 26529344]
HEK293	IC₅₀	1.47 nM Compound: 2; PSNCBAM-1	Inverse agonist activity at human CB1 receptor expressed in HEK293 cell membranes assessed as suppression of [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method Inverse agonist activity at human CB1 receptor expressed in HEK293 cell membranes assessed as suppression of [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method	[PMID: 31596583]
HEK293	EC₅₀	167 nM Compound: 4, PSNCBAM-1	Displacement of [3H]CP55,940 from human CB1 receptor expressed in HEK293 cells after 1 hr by scintillation counting Displacement of [3H]CP55,940 from human CB1 receptor expressed in HEK293 cells after 1 hr by scintillation counting	[PMID: 25162172]
HEK293	IC₅₀	2620 nM Compound: 2; PSNCBAM-1	Allosteric modulator activity at human CB1 receptor expressed in HEK293 cells assessed as suppression of 100 nM CP55,940-induced reduction in forskolin-stimulated cAMP production pre-incubated for 25 mins before forskolin and CP55,940 addition and measure Allosteric modulator activity at human CB1 receptor expressed in HEK293 cells assessed as suppression of 100 nM CP55,940-induced reduction in forskolin-stimulated cAMP production pre-incubated for 25 mins before forskolin and CP55,940 addition and measure	[PMID: 31596583]
HEK293	IC₅₀	455 nM Compound: 2; PSNCBAM-1	Allosteric modulator activity at human CB1 receptor expressed in HEK293 cell membranes assessed as suppression of 100 nM CP55,940-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method Allosteric modulator activity at human CB1 receptor expressed in HEK293 cell membranes assessed as suppression of 100 nM CP55,940-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method	[PMID: 31596583]
U-937	IC₅₀	> 10 μM Compound: PSNCBAM-1	Inhibition of [ethanolamine-1-3H]AEA uptake in human U937 cell homogenate preincubated for 20 mins followed by AEA addition measured after 5 mins by scintillation counting method Inhibition of [ethanolamine-1-3H]AEA uptake in human U937 cell homogenate preincubated for 20 mins followed by AEA addition measured after 5 mins by scintillation counting method	[PMID: 29079014]

Molecular Weight

392.88

Formula

C₂₂H₂₁ClN₄O

CAS No.

877202-74-9

Appearance

Solid

Color

White to off-white

SMILES

ClC(C=C1)=CC=C1NC(NC2=CC=CC(C3=CC=CC(N4CCCC4)=N3)=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (318.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5453 mL	12.7265 mL	25.4531 mL
5 mM	0.5091 mL	2.5453 mL	5.0906 mL
10 mM	0.2545 mL	1.2727 mL	2.5453 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.48%

Select Batch:

Data Sheet (272 KB) SDS (393 KB)

COA (249 KB) HNMR (271 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Horswill JG, et al. PSNCBAM-1, a novel allosteric antagonist at cannabinoid CB1 receptors with hypophagic effects in rats. Br J Pharmacol. 2007 Nov;152(5):805-14. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5453 mL	12.7265 mL	25.4531 mL	63.6327 mL
	5 mM	0.5091 mL	2.5453 mL	5.0906 mL	12.7265 mL
	10 mM	0.2545 mL	1.2727 mL	2.5453 mL	6.3633 mL
	15 mM	0.1697 mL	0.8484 mL	1.6969 mL	4.2422 mL
	20 mM	0.1273 mL	0.6363 mL	1.2727 mL	3.1816 mL
	25 mM	0.1018 mL	0.5091 mL	1.0181 mL	2.5453 mL
	30 mM	0.0848 mL	0.4242 mL	0.8484 mL	2.1211 mL
	40 mM	0.0636 mL	0.3182 mL	0.6363 mL	1.5908 mL
	50 mM	0.0509 mL	0.2545 mL	0.5091 mL	1.2727 mL
	60 mM	0.0424 mL	0.2121 mL	0.4242 mL	1.0605 mL
	80 mM	0.0318 mL	0.1591 mL	0.3182 mL	0.7954 mL
	100 mM	0.0255 mL	0.1273 mL	0.2545 mL	0.6363 mL

PSNCBAM-1 Related Classifications

Metabolic Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PSNCBAM-1877202-74-9PSNCBAM1PSNCBAM 1Cannabinoid ReceptorInhibitorinhibitorinhibit

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