| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| 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].
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|---|---|
| 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].
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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. |
| References |
[1]. F Wunder, et al. 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.
[2]. Q J Shi, et al. HAMI 3379, a CysLT2R antagonist, dose- and time-dependently attenuates brain injury and inhibits microglial inflammation after focal cerebral ischemia in rats. Neuroscience. 2015 Apr 16;291:53-69. |
| Molecular Formula |
C34H45NO8
|
|---|---|
| Molecular Weight |
595.733
|
| CAS # |
1245653-57-9
|
| Related CAS # |
(Rac)-HAMI 3379;712313-35-4
|
| 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
|
| 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)
|
| 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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