Clobenpropit

Cat. No.: HY-115447: FAQs
Data Sheet Handling Instructions

Molarity Calculator

Clobenpropit is a potent histamine H3-receptor antagonist. Clobenpropit decreases dopamine release and increases histamine levels in the hypothalamus. Clobenpropit shows antipsychotic-like activities. Clobenpropit causes a resuscitating effect in rats subjected to the hemorrhagic shock.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Clobenpropit dihydrobromide) usually boasts enhanced water solubility and stability.

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

Clobenpropit Chemical Structure

CAS No. : 145231-45-4

Size		Stock
MOQ		Minimum order quantity
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote
Other size		Get quote

Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other Forms of Clobenpropit:

Clobenpropit dihydrobromide Get quote

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All Histamine Receptor Isoform Specific Products:

View All Isoforms

H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

H₃ receptor

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	1.7 nM Compound: clobenpropit	Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay	[PMID: 19553110]
HT-1080	IC₅₀	1 nM Compound: Clobenpropit	Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay	[PMID: 20833043]
HT-1080	IC₅₀	1 nM Compound: Clobenpropit	Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay	[PMID: 20833043]

In Vivo

Clobenpropit (15 mg/kg; i.p.; once daily for 7 days) counteracts the modulatory effects of MK-801 (HY-15084B) on dopamine and histamine levels and prevents MK-801-induced hyper locomotor behaviors^[1].
Clobenpropit (1, 2, 5 μmoL/kg; i.v.) causes a resuscitating effect in rats subjected to the hemorrhagic shock^[2].

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

Animal Model:	150-200g, 12-week-old male wistar albino rats^[1]
Dosage:	15 mg/kg
Administration:	I.p.; once daily for 7 days
Result:	Exhibited a significant reduction of hyperlocomotor activities induced by a single-dose administration of MK-801 (0.2 mg/kg, i.p.), and reduced the MK-801-induced dopamine release, exhibited further increase in histamine levels in the hypothalamus.

Animal Model:	205-470g, adult male Wistar rats^[2]
Dosage:	1, 2, 5 μmoL/kg (after 6-hydroxydopamine (50 mg/kg (SC) for 3 consecutive days)
Administration:	I.v.
Result:	Triggered a statistically significant increase of mean arterial pressure (MAP) (dose 2 μmol/kg) and heart rate (HR) (doses of 1, 2, 5 μmol/kg).

Molecular Weight

308.83

Formula

C₁₄H₁₇ClN₄S

CAS No.

145231-45-4

SMILES

N=C(SCCCC1=CN=CN1)NCC2=CC=C(Cl)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Mahmood D, et al. The Effect of Subchronic Dosing of Ciproxifan and Clobenpropit on Dopamine and Histamine Levels in Rats. J Exp Neurosci. 2015 Aug 31;9:73-80. [Content Brief]

[2]. Wanot B, et al. Cardiovascular effects of H3 histamine receptor inverse agonist/ H4 histamine receptor agonist, clobenpropit, in hemorrhage-shocked rats. PLoS One. 2018 Aug 2;13(8):e0201519. [Content Brief]

Clobenpropit Related Classifications

Neurological Disease

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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:

Clobenpropit145231-45-4Histamine Receptordopaminehistamineantipsychotic-likehemorrhagic shockMAPHRInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks