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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
ln Vitro |
With an IC50 of 560 nM, LOE 908 hydrochloride inhibits cation conductance in a concentration-dependent manner. Voltage-dependent Ca2+ channels with an IC50 of 28 μM block dihydropyride-sensitive Ba2+ currents in voltage-clamped A7r5 cells [1].
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ln Vivo |
In rats with acute neuromotor dysfunction, LOE 908 (4 or 2 mg/kg followed by 160 or 80 mg/kg; iv) hydrochloride can lessen the dysfunction[2].
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Animal Protocol |
Animal/Disease Models: Adult male SD (Sprague-Dawley) rats, lateral fluid percussion brain injury model[2]
Doses: 4 mg/kg bolus followed by 160 mg/kg over 24 h or 2 mg/kg bolus followed by 80 mg/kg over 24 h Route of Administration: intravenous (iv) administration Experimental Results: Dramatically improved neuromotor function at 48 h postinjury when compared to vehicle treatment. |
References |
[1]. Krautwurst D, et al. The isoquinoline derivative LOE 908 selectively blocks vasopressin-activated nonselective cation currents in A7r5 aortic smooth muscle cells. Naunyn Schmiedebergs Arch Pharmacol. 1994 Mar;349(3):301-7.
[2]. Cheney JA, et al. The novel compound LOE 908 attenuates acute neuromotor dysfunction but not cognitive impairment or cortical tissue loss following traumatic brain injury in rats. J Neurotrauma. 2000 Jan;17(1):83-91. |
Molecular Formula |
C41H49CLN2O9
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Molecular Weight |
749.29
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CAS # |
143482-60-4
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SMILES |
Cl.O=C(C(C1C=CC=CC=1)C1C2C=C(C(=CC=2CCN=1)OC)OC)N(CCC1C=CC(=C(C=1OC)OC)OC)CCC1C=CC(=C(C=1OC)OC)OC
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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 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.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.3346 mL | 6.6730 mL | 13.3460 mL | |
5 mM | 0.2669 mL | 1.3346 mL | 2.6692 mL | |
10 mM | 0.1335 mL | 0.6673 mL | 1.3346 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.