| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
HAMI-3379 targets the cysteinyl leukotriene receptor 2 (CysLT2), a G protein-coupled receptor that mediates the effects of cysteinyl leukotrienes (CysLTs: LTC4, LTD4, and LTE4). The CysLT2 receptor is involved in inflammatory responses and is expressed on various cell types, including immune cells and cells in the central nervous system. By blocking this receptor, HAMI-3379 inhibits CysLT-mediated signaling, reducing inflammation and providing neuroprotection.
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| ln Vitro |
With IC50 values of 3.8 nM and 4.4 nM, respectively, HAMI3379 inhibited leukotriene D4- (LTD4-) and leukotriene C4- (LTC4-)-induced intracellular calcium mobilization in the CysLT2 receptor reporter cell line. HAMI3379's efficacy against recombinant CysLT1 receptor cell lines is extremely poor (IC50>10000 nM). There is no agonistic activity shown by HAMI3379 on either CysLT receptor cell line [1].
In vitro, HAMI-3379 is a potent and selective CysLT2 receptor antagonist with an IC50 of 37.9 nM. It displays high selectivity for CysLT2 over CysLT1 (IC50 >30 µM). In microglial cell models, it reduces inflammation, suggesting its potential to attenuate neuroinflammation. It enhances astrocyte-related factors, which may contribute to its neuroprotective effects. |
| ln Vivo |
HAMI 3379 (0.025-0.4 mg/kg; i.p.) 0.1-0.4 mg/kg considerably lowers the percentage rise in infarct volume and ischemic/contralateral hemisphere ratio [2]. HAMI3379 (0.1 mg/kg; intraperitoneal injection) administered at 0 and 1 hour after reperfusion reduced infarct volume, reduced cerebral edema, decreased neurological scores, and increased grip angle [2].
In vivo, HAMI-3379 has demonstrated protective effects in models of acute and subacute ischemic brain injury. In a rat model of focal cerebral ischemia, intraperitoneal administration of 0.1-0.4 mg/kg significantly reduced infarct volume and the percentage increase in the ischemic/contralateral hemisphere ratio. It also attenuates microglia-related inflammation in the brain. |
| Enzyme Assay |
The inhibitory activity of HAMI-3379 is assessed using radioligand binding assays, where its IC50 for CysLT2 is determined. Its selectivity is confirmed by testing it against CysLT1 and other related receptors. Functional activity can be assessed using cell-based assays measuring calcium mobilization or other downstream signaling events.
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| Cell Assay |
The cellular activity of HAMI-3379 is evaluated in cells expressing CysLT2, such as microglia or other immune cells. Cells are treated with the compound, and its effect on CysLT-induced signaling and inflammatory mediator production is assessed. Its neuroprotective effects can be studied in neuronal cell cultures under conditions of oxidative stress or inflammation.
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats (250-300 g) after MCAO [2]
Doses: 0.025, 0.05, 0.1, 0.2, 0.4 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Significant reduction in infarct volume and The ischemic/contralateral infarct area percentage increase hemispheric ratio (brain edema index) is 0.1-0.4 mg/kg. Dramatically diminished neurological deficit scores. In animal studies, HAMI-3379 is typically administered via intraperitoneal (i.p.) injection. In models of ischemic brain injury, it is given before or after the induction of ischemia. Efficacy endpoints include infarct volume, neurological deficit scores, and markers of inflammation and oxidative stress in brain tissue. |
| ADME/Pharmacokinetics |
Detailed pharmacokinetic properties of HAMI-3379 are not extensively documented. As a small molecule (MW 595.72), it is likely to have moderate bioavailability. Its solubility in DMSO facilitates formulation for in vivo administration. Its use in animal models at doses of 0.1-0.4 mg/kg indicates it is active at low concentrations.
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| Toxicity/Toxicokinetics |
Toxicology data for HAMI-3379 is limited. As a potent antagonist of a receptor involved in inflammation, its safety profile is a consideration for any therapeutic application. However, its use in research models suggests it is tolerated at the doses used for efficacy studies.
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| References |
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| Additional Infomation |
HAMI-3379 (CAS: 1245653-57-9) is a valuable research tool for studying the role of the CysLT2 receptor in inflammation and neuroprotection. Its high potency and selectivity make it a key compound for investigating the therapeutic potential of CysLT2 antagonists in conditions such as stroke, neuroinflammation, and other inflammatory diseases.
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| Molecular Formula |
C34H45NO8
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|---|---|
| Molecular Weight |
595.733
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| Exact Mass |
595.314
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| CAS # |
1245653-57-9
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| Related CAS # |
(Rac)-HAMI 3379;712313-35-4
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| PubChem CID |
91523600
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| Appearance |
White to off-white solid powder
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| LogP |
6.2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
43
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| Complexity |
853
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O(CCCCOC1C=CC(=CC=1)CCCOC1=CC=C(C(=O)O)C=C1C(N[C@@H]1CCC[C@@H](C(=O)O)C1)=O)C1CCCCC1
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| InChi Key |
HRJWSEPIRZRGCL-BDYUSTAISA-N
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| 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)/t25-,27-/m0/s1
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| Chemical Name |
3-[[(1S,3S)-3-carboxycyclohexyl]carbamoyl]-4-[3-[4-(4-cyclohexyloxybutoxy)phenyl]propoxy]benzoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~167.86 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6786 mL | 8.3931 mL | 16.7861 mL | |
| 5 mM | 0.3357 mL | 1.6786 mL | 3.3572 mL | |
| 10 mM | 0.1679 mL | 0.8393 mL | 1.6786 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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