WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H522492
CAS#: 712313-35-4
Description: 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.
Hodoodo Cat#: H522492
Name: HAMI3379
CAS#: 712313-35-4
Chemical Formula: C34H45NO8
Exact Mass: 595.31
Molecular Weight: 595.733
Elemental Analysis: C, 68.55; H, 7.61; N, 2.35; O, 21.48
Synonym: HAMI3379; HAMI-3379; 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: >95 % (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:
Biological target: | |
In vitro activity: | |
In vivo activity: |
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: | |
In vitro protocol: | |
In vivo protocol: |
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.