HAMI3379 | CAS#712313-35-4 | CysLT2 receptor antagonist

MedKoo Cat#: 522492 | Name: HAMI3379

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

HAMI 3379 is a selective CysLT2 receptor antagonist. HAMI 3379 protects against acute brain injury after focal cerebral ischemia in rats. HAMI 3379 attenuates ischemia-like neuronal injury by inhibiting microglial activation. HAMI 3379 effectively blocked CysLT2R-mediated microglial activation, thereby indirectly attenuating ischemic neuronal injury. Therefore, CysLT2R antagonists may represent a new type of therapeutic agent in the treatment of ischemic stroke.

Chemical Structure

HAMI3379

CAS#712313-35-4

Theoretical Analysis

MedKoo Cat#: 522492

Name: HAMI3379

CAS#: 712313-35-4

Chemical Formula: C34H45NO8

Exact Mass: 595.3145

Molecular Weight: 595.73

Elemental Analysis: C, 68.55; H, 7.61; N, 2.35; O, 21.48

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 550.00	2 Weeks
10mg	USD 950.00	2 Weeks

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Synonym

HAMI3379; HAMI-3379; HAMI 3379; (Rac)-HAMI 3379

IUPAC/Chemical Name

3-[[(3-carboxycyclohexyl)amino]carbonyl]-4-[3-[4-[4-(cyclohexyloxy)butoxy]phenyl]propoxy]-benzoic acid

InChi Key

HRJWSEPIRZRGCL-UHFFFAOYSA-N

InChi Code

InChI=1S/C34H45NO8/c36-32(35-27-10-6-9-25(22-27)33(37)38)30-23-26(34(39)40)15-18-31(30)43-21-7-8-24-13-16-29(17-14-24)42-20-5-4-19-41-28-11-2-1-3-12-28/h13-18,23,25,27-28H,1-12,19-22H2,(H,35,36)(H,37,38)(H,39,40)

SMILES Code

O=C(O)C1=CC=C(OCCCC2=CC=C(OCCCCOC3CCCCC3)C=C2)C(C(NC4CC(C(O)=O)CCC4)=O)=C1

Appearance

Solid powder

Purity

>90 % (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, not in water

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

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#C8M10C31

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

HAMI 3379 is a potent and selective Cysteinyl leukotriene (CysLT2) receptor antagonist.

In vitro activity:

In binding studies using membranes from the CysLT(2) and CysLT(1) receptor cell lines, HAMI3379 inhibited [(3)H]-LTD(4) binding with IC(50) values of 38 nM and >10 000 nM respectively. In isolated Langendorff-perfused guinea pig hearts HAMI3379 concentration-dependently inhibited and reversed the LTC(4)-induced perfusion pressure increase and contractility decrease. HAMI3379 was identified as a potent and selective CysLT(2) receptor antagonist, which was devoid of CysLT receptor agonism. Reference: Br J Pharmacol. 2010 May;160(2):399-409. https://pubmed.ncbi.nlm.nih.gov/20423349/

In vivo activity:

In contrast to the PSD group, HM3379 significantly ameliorated PSD-induced neuronal loss (1441.00 ± 21.71 vs. 1184.00 ± 26.90, p < 0.05; Figure 1G,H). In addition, HM3379 treatment diminished the number of TUNEL-positive cells in the cerebral cortex of the PSD group (Figure 2A). These results reveal that HM3379 can ameliorate depression-like behaviors and neurological injury in the PSD model of gerbils. Reference: Brain Sci. 2022 Jul 24;12(8):976. https://pubmed.ncbi.nlm.nih.gov/35892417/

	Solvent	mg/mL	mM
Solubility
	DMF	20.0	33.57
	DMF:PBS (pH 7.2) (1:1)	0.5	0.84
	DMSO	60.0	100.72
	Ethanol	5.0	8.39

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 595.73 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.

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:

1. Merten N, Fischer J, Simon K, Zhang L, Schröder R, Peters L, Letombe AG, Hennen S, Schrage R, Bödefeld T, Vermeiren C, Gillard M, Mohr K, Lu QR, Brüstle O, Gomeza J, Kostenis E. Repurposing HAMI3379 to Block GPR17 and Promote Rodent and Human Oligodendrocyte Differentiation. Cell Chem Biol. 2018 Jun 21;25(6):775-786.e5. doi: 10.1016/j.chembiol.2018.03.012. Epub 2018 Apr 26. PMID: 29706593; PMCID: PMC6685917. 2. Wunder F, Tinel H, Kast R, Geerts A, Becker EM, Kolkhof P, Hütter J, Ergüden J, Härter M. Pharmacological characterization of the first potent and selective antagonist at the cysteinyl leukotriene 2 (CysLT(2)) receptor. Br J Pharmacol. 2010 May;160(2):399-409. doi: 10.1111/j.1476-5381.2010.00730.x. PMID: 20423349; PMCID: PMC2874861. 3. Zhou L, Zhang J, Han X, Fang J, Zhou S, Lu L, Shi Q, Ying H. CysLT2R Antagonist HAMI 3379 Ameliorates Post-Stroke Depression through NLRP3 Inflammasome/Pyroptosis Pathway in Gerbils. Brain Sci. 2022 Jul 24;12(8):976. doi: 10.3390/brainsci12080976. PMID: 35892417; PMCID: PMC9330558.

In vitro protocol:

In vivo protocol:

1. Zhou L, Zhang J, Han X, Fang J, Zhou S, Lu L, Shi Q, Ying H. CysLT2R Antagonist HAMI 3379 Ameliorates Post-Stroke Depression through NLRP3 Inflammasome/Pyroptosis Pathway in Gerbils. Brain Sci. 2022 Jul 24;12(8):976. doi: 10.3390/brainsci12080976. PMID: 35892417; PMCID: PMC9330558.

1: Xu DM, Zhang XY, Wang XR, Chen L, Zhang LH, Shi QJ, Fang SH, Lu YB, Zhang WP, Wei EQ. [Antioxidative effects of cysteinyl leukotriene receptor antagonists montelukast and HAMI 3379 on ischemic injury in rat cortical neurons in vitro]. Zhejiang Da Xue Xue Bao Yi Xue Ban. 2014 May;43(3):257-64. Chinese. PubMed PMID: 24998647. 2: Lin K, Fang S, Cai B, Huang X, Zhang X, Lu Y, Zhang W, Wei E. ERK/Egr-1 signaling pathway is involved in CysLT2 receptor-mediated IL-8 production in HEK293 cells. Eur J Cell Biol. 2014 Jul;93(7):278-88. doi: 10.1016/j.ejcb.2014.05.001. Epub 2014 May 20. PubMed PMID: 24925646. 3: Zhang Z, Luo J, Huang J, Liu Z, Fang S, Zhang WP, Wei E, Lu Y. [Leukotriene D4 activates BV2 microglia in vitro]. Zhejiang Da Xue Xue Bao Yi Xue Ban. 2013 May;42(3):253-60. Chinese. PubMed PMID: 23801612. 4: Zhang XY, Wang XR, Xu DM, Yu SY, Shi QJ, Zhang LH, Chen L, Fang SH, Lu YB, Zhang WP, Wei EQ. HAMI 3379, a CysLT2 receptor antagonist, attenuates ischemia-like neuronal injury by inhibiting microglial activation. J Pharmacol Exp Ther. 2013 Aug;346(2):328-41. doi: 10.1124/jpet.113.203604. Epub 2013 Jun 7. PubMed PMID: 23750020. 5: Dong X, Zhao Y, Huang X, Lin K, Chen J, Wei E, Liu T, Hu Y. Structure-based drug design using GPCR homology modeling: toward the discovery of novel selective CysLT2 antagonists. Eur J Med Chem. 2013 Apr;62:754-63. doi: 10.1016/j.ejmech.2013.01.041. Epub 2013 Feb 9. PubMed PMID: 23455026. 6: Shi QJ, Xiao L, Zhao B, Zhang XY, Wang XR, Xu DM, Yu SY, Fang SH, Lu YB, Zhang WP, Sa XY, Wei EQ. Intracerebroventricular injection of HAMI 3379, a selective cysteinyl leukotriene receptor 2 antagonist, protects against acute brain injury after focal cerebral ischemia in rats. Brain Res. 2012 Nov 12;1484:57-67. doi: 10.1016/j.brainres.2012.09.020. Epub 2012 Sep 18. PubMed PMID: 23000196. 7: Wunder F, Tinel H, Kast R, Geerts A, Becker EM, Kolkhof P, Hütter J, Ergüden J, Härter M. Pharmacological characterization of the first potent and selective antagonist at the cysteinyl leukotriene 2 (CysLT(2)) receptor. Br J Pharmacol. 2010 May;160(2):399-409. doi: 10.1111/j.1476-5381.2010.00730.x. PubMed PMID: 20423349; PubMed Central PMCID: PMC2874861.