N-(4-CHLOROBENZYL)-S-[3-(4(5)-IMIDAZOLYL)PROPYL]ISOTHIOUREA CAS#: 145231-35-2

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N-(4-CHLOROBENZYL)-S-[3-(4(5)-IMIDAZOLYL)PROPYL]ISOTHIOUREA

Basic information Safety Supplier Related

N-(4-CHLOROBENZYL)-S-[3-(4(5)-IMIDAZOLYL)PROPYL]ISOTHIOUREA Basic information

Product Name:

N-(4-CHLOROBENZYL)-S-[3-(4(5)-IMIDAZOLYL)PROPYL]ISOTHIOUREA

Synonyms:

Clobenpropit (hydrobromide)
Clobenpropit dihydrobromide Solution, 100ppm
Clobenpropit dihydrobromide Solution, 1000ppm
3-(1H-Imidazol-4-yl)propyl 4-Chlorobenzylcarbamimidothioate Dihydrobromide
Apoptosis,inhibit,Clobenpropit dihydrobromide,histamine H3R,antagonist,inverse,Inhibitor,pancreatic,agonist,cancer,H3LR,Histamine Receptor
Clobenpropit dihydrobromide, H3 antagonist

CAS:

145231-35-2

MF:

C14H17ClN4S.2BrH

MW:

470.659

Mol File:

145231-35-2.mol

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N-(4-CHLOROBENZYL)-S-[3-(4(5)-IMIDAZOLYL)PROPYL]ISOTHIOUREA Chemical Properties

Melting point:: 205°C(lit.)
storage temp.: Store at -20°C
solubility: DMSO: 30 mg/ml; Ethanol: 2.5 mg/ml; Water: 20 mg/ml
form: powder to crystal
color: White to Gray to Red
Water Solubility: Soluble to 100 mM in water

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Safety Information

HS Code: 2933.29.4300

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N-(4-CHLOROBENZYL)-S-[3-(4(5)-IMIDAZOLYL)PROPYL]ISOTHIOUREA Usage And Synthesis

Uses

Clobenpropit Dihydrobromide and it’s analogues functions as potent histamine H3 antagonist.

Definition

ChEBI: A hydrobromide salt obtained by reaction of clobenpropit with two equivalents of hydrobromic acid. An extremely potent histamine H3 antagonist/inverse agonist (pA2 = 9.93). Also displays partial agonist activity at H4 receptors; induces eosinophil shape change with an EC50 of 3 nM.

in vivo

The combination treatment of Clobenpropit (every other day intraperitoneal injection at 20 μM per kilogram for 40 d) and Gemcitabine (twice-a-week intraperitoneal injection at 125 mg/kg for 40 d) shows significant tumor growth inhibition^[3].

Animal Model:	Five-week-old male BALB/c nude mice with Panc-1 xenograft^[3]
Dosage:	20 μM per kilogram
Administration:	Intraperitoneal injection; every other day for 40 days. Gemcitabine (twice-a-week intraperitoneal injection at 125 mg/kg for 40 d)
Result:	The combination treatment showed significant tumor growth inhibition compared with other treatment groups (control 501±92 mg, Gemcitabine 294±46 mg, Clobenpropit 444±167 mg, and combination 154±54 mg).

IC 50

Human H3LR: 9.44 (pKi); Rat H3LR: 9.75 (pKi); H₄ receptor: 13 nM (Ki); H₂ Receptor: 5.6 (pKi)

storage

Store at RT

N-(4-CHLOROBENZYL)-S-[3-(4(5)-IMIDAZOLYL)PROPYL]ISOTHIOUREASupplier

TOKYO CHEMICAL INDUSTRY CO., LTD.

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Alta Scientific Co., Ltd.

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Shanghai EFE Biological Technology Co., Ltd.

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Email: info@efebio.com

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