Clobenpropit free base

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MedKoo CAT#: 413095

CAS#: 145231-45-4 (free base)

Description: Clobenpropit, also known as VUF 9153, is a highly potent H3 antagonist and H4 partial agonist. Clobenpropit has been shown to protect NMDA-induced neuronal necrosis in cortical neuronal cell culture from rats. Clobenpropit promises neuroprotection against LPS-induced cognitive deficits by meliorating neuroinflammation and restoring the MRCC enzymes in mice. Clobenpropit protects propofol-induced apoptosis of hippocampal neurons through PI3K/AKT pathway.

Chemical Structure

Clobenpropit free base
CAS# 145231-45-4 (free base)

Theoretical Analysis

MedKoo Cat#: 413095
Name: Clobenpropit free base
CAS#: 145231-45-4 (free base)
Chemical Formula: C14H17ClN4S
Exact Mass: 308.09
Molecular Weight: 308.830
Elemental Analysis: C, 54.45; H, 5.55; Cl, 11.48; N, 18.14; S, 10.38

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales or click below button.
Note: Price will be listed if it is available in the future.

Related CAS #: 145231-45-4 (free base)   145231-35-2 (2HBr),  

Synonym: Clobenpropit (free base); VUF9153; VUF-9153; VUF 9153

IUPAC/Chemical Name: Carbamimidothioic acid, ((4-chlorophenyl)methyl)-, 3-(1H-imidazol-4-yl)propyl ester


InChi Code: InChI=1S/C14H17ClN4S/c15-12-5-3-11(4-6-12)8-18-14(16)20-7-1-2-13-9-17-10-19-13/h3-6,9-10H,1-2,7-8H2,(H2,16,18)(H,17,19)


Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 308.83 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Mani V, Arfeen M, Ali HM, Abdel-Moneim AH, Aldubayan M, Alhowail A. Neuroprotective Effect of Clobenpropit against Lipopolysaccharide-Induced Cognitive Deficits via Attenuating Neuroinflammation and Enhancing Mitochondrial Functions in Mice. Brain Sci. 2021 Dec 8;11(12):1617. doi: 10.3390/brainsci11121617. PMID: 34942919; PMCID: PMC8699680.

2: Sharma A, Muresanu DF, Patnaik R, Menon PK, Tian ZR, Sahib S, Castellani RJ, Nozari A, Lafuente JV, Buzoianu AD, Skaper SD, Bryukhovetskiy I, Manzhulo I, Wiklund L, Sharma HS. Histamine H3 and H4 receptors modulate Parkinson's disease induced brain pathology. Neuroprotective effects of nanowired BF-2649 and clobenpropit with anti-histamine-antibody therapy. Prog Brain Res. 2021;266:1-73. doi: 10.1016/bs.pbr.2021.06.003. Epub 2021 Oct 6. PMID: 34689857.

3: He W, Yuan QH, Zhou Q. Histamine H3 receptor antagonist Clobenpropit protects propofol-induced apoptosis of hippocampal neurons through PI3K/AKT pathway. Eur Rev Med Pharmacol Sci. 2018 Nov;22(22):8013-8020. doi: 10.26355/eurrev_201811_16430. PMID: 30536350.

4: Wanot B, Jasikowska K, Niewiadomska E, Biskupek-Wanot A. 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. doi: 10.1371/journal.pone.0201519. PMID: 30071054; PMCID: PMC6072086.

5: Mena-Avila E, Márquez-Gómez R, Aquino-Miranda G, Nieto-Alamilla G, Arias- Montaño JA. Clobenpropit, a histamine H3 receptor antagonist/inverse agonist, inhibits [3H]-dopamine uptake by human neuroblastoma SH-SY5Y cells and rat brain synaptosomes. Pharmacol Rep. 2018 Feb;70(1):146-155. doi: 10.1016/j.pharep.2017.08.007. Epub 2017 Aug 30. PMID: 29414147.

6: Patnaik R, Sharma A, Skaper SD, Muresanu DF, Lafuente JV, Castellani RJ, Nozari A, Sharma HS. Histamine H3 Inverse Agonist BF 2649 or Antagonist with Partial H4 Agonist Activity Clobenpropit Reduces Amyloid Beta Peptide-Induced Brain Pathology in Alzheimer's Disease. Mol Neurobiol. 2018 Jan;55(1):312-321. doi: 10.1007/s12035-017-0743-8. PMID: 28861757.

7: Tanaka T, Kochi T, Shirakami Y, Mori T, Niwa A, Watanabe N, Moriwaki H, Shimizu M. Erratum: Tanaka, T. et al. Cimetidine and Clobenpropit Attenuate Inflammation-Associated Colorectal Carcinogenesis in Male ICR Mice. Cancers, 2016, 8, 25. Cancers (Basel). 2017 Jul 5;9(7):80. doi: 10.3390/cancers9070080. Erratum for: Cancers (Basel). 2016 Feb 20;8(2):null. PMID: 28678152; PMCID: PMC5532616.

8: Tanaka T, Kochi T, Shirakami Y, Mori T, Kurata A, Watanabe N, Moriwaki H, Shimizu M. Cimetidine and Clobenpropit Attenuate Inflammation-Associated Colorectal Carcinogenesis in Male ICR Mice. Cancers (Basel). 2016 Feb 20;8(2):25. doi: 10.3390/cancers8020025. Erratum in: Cancers (Basel). 2017 Jul 05;9(7): PMID: 26907350; PMCID: PMC4773748.

9: Mahmood D, Pillai KK, Khanam R, Jahan K, Goswami D, Akhtar M. 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. doi: 10.4137/JEN.S27244. PMID: 26379444; PMCID: PMC4556212.

10: Femenía T, Magara S, DuPont CM, Lindskog M. Hippocampal-Dependent Antidepressant Action of the H3 Receptor Antagonist Clobenpropit in a Rat Model of Depression. Int J Neuropsychopharmacol. 2015 Mar 11;18(9):pyv032. doi: 10.1093/ijnp/pyv032. PMID: 25762718; PMCID: PMC4576519.

11: Paik WH, Ryu JK, Jeong KS, Park JM, Song BJ, Lee SH, Kim YT, Yoon YB. Clobenpropit enhances anti-tumor effect of gemcitabine in pancreatic cancer. World J Gastroenterol. 2014 Jul 14;20(26):8545-57. doi: 10.3748/wjg.v20.i26.8545. PMID: 25024609; PMCID: PMC4093704.

12: Meng F, Han Y, Staloch D, Francis T, Stokes A, Francis H. The H4 histamine receptor agonist, clobenpropit, suppresses human cholangiocarcinoma progression by disruption of epithelial mesenchymal transition and tumor metastasis. Hepatology. 2011 Nov;54(5):1718-28. doi: 10.1002/hep.24573. PMID: 21793031.

13: Uma Devi P, Manocha A, Khanam R, Vohora D. Beneficial interaction between clobenpropit and pyridoxine in prevention of electroshock-induced seizures in mice: lack of histaminergic mechanisms. Hum Exp Toxicol. 2011 Jan;30(1):84-8. doi: 10.1177/0960327110372398. Epub 2010 May 28. PMID: 20511290.

14: Fu Q, Dai H, He P, Hu W, Fan Y, Zhang W, Chen Z. The H3 receptor antagonist clobenpropit protects against Abeta42-induced neurotoxicity in differentiated rat PC12 cells. Pharmazie. 2010 Apr;65(4):257-60. PMID: 20432621.

15: Hansen KB, Mullasseril P, Dawit S, Kurtkaya NL, Yuan H, Vance KM, Orr AG, Kvist T, Ogden KK, Le P, Vellano KM, Lewis I, Kurtkaya S, Du Y, Qui M, Murphy TJ, Snyder JP, Bräuner-Osborne H, Traynelis SF. Implementation of a fluorescence-based screening assay identifies histamine H3 receptor antagonists clobenpropit and iodophenpropit as subunit-selective N-methyl-D-aspartate receptor antagonists. J Pharmacol Exp Ther. 2010 Jun;333(3):650-62. doi: 10.1124/jpet.110.166256. Epub 2010 Mar 2. PMID: 20197375; PMCID: PMC2879924.

16: Wang HJ, Lu M, Gong YX, Chen Z. [Effects of clobenpropit and histidine on reinstatement of morphine-induced conditioned place preference]. Zhejiang Da Xue Xue Bao Yi Xue Ban. 2009 Nov;38(6):559-64. Chinese. doi: 10.3785/j.issn.1008-9292.2009.06.002. PMID: 20014479.

17: Lim HD, Istyastono EP, van de Stolpe A, Romeo G, Gobbi S, Schepers M, Lahaye R, Menge WM, Zuiderveld OP, Jongejan A, Smits RA, Bakker RA, Haaksma EE, Leurs R, de Esch IJ. Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies. Bioorg Med Chem. 2009 Jun 1;17(11):3987-94. doi: 10.1016/j.bmc.2009.04.007. Epub 2009 Apr 11. PMID: 19414267.

18: Yoneyama H, Shimoda A, Araki L, Hatano K, Sakamoto Y, Kurihara T, Yamatodani A, Harusawa S. Efficient approaches to S-alkyl-N-alkylisothioureas: syntheses of histamine H3 antagonist clobenpropit and its analogues. J Org Chem. 2008 Mar 21;73(6):2096-104. doi: 10.1021/jo702181x. Epub 2008 Feb 16. PMID: 18278935.

19: Dai H, Fu Q, Shen Y, Hu W, Zhang Z, Timmerman H, Leurs R, Chen Z. The histamine H3 receptor antagonist clobenpropit enhances GABA release to protect against NMDA-induced excitotoxicity through the cAMP/protein kinase A pathway in cultured cortical neurons. Eur J Pharmacol. 2007 Jun 1;563(1-3):117-23. doi: 10.1016/j.ejphar.2007.01.069. Epub 2007 Feb 8. PMID: 17350613.

20: Shenton FC, Chazot PL. Probing the importance of N-glycosylation for [(3)H] clobenpropit binding to human H (3) receptors expressed in HEK 293 cells . 3. Molecular and chemical aspects of the histamine receptors. Inflamm Res. 2006 Apr;55 Suppl 1:S40-1. doi: 10.1007/s00011-005-0033-1. PMID: 16547815.