| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
OPC-28326 stimulates microvessel development and improves endothelial tube formation. OPC-28326 does not alter the overall levels of eNOS or Akt, but it does cause the phosphorylation of these molecules in HAEC in a dose-dependent manner [1]. Yohimbine (10-1000 nM) and OPC-28326 (1-100 μM) elicit a rightward shift in the clonidine concentration-response curve [2].
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|---|---|
| ln Vivo |
OPC-28326 improves the recovery of blood flow in mice suffering from hindlimb ischemia. The ischemic leg's histologically detectable capillary count is markedly increased by OPC-28326. In eNOS−/− mice, OPC-28326 had no therapeutic effects on blood flow restoration [1]. Yohimbine and OPC-28326 (3–30 mg/kg, i.v.) generate a dose-dependent rightward change in the pressor dose–response curve induced by B-HT 920. OPC-28326 has no effect on rats' mydriasis [2].
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| References |
[1]. Sumi M, et al. OPC-28326, a selective femoral arterial vasodilator, augments ischemia induced angiogenesis. Biomed Pharmacother. 2007 May;61(4):209-15. Epub 2006 Dec 28.
[2]. Orito K, et al. alpha(2)-adrenoceptor antagonist properties of OPC-28326, a novel selective peripheral vasodilator. Br J Pharmacol. 2001 Oct;134(4):763-70 |
| Additional Infomation |
At low doses, OPC 28326 selectively vasodilates the femoral arterial bed due to its inhibitory action at alpha-2-adrenoceptors while having minimal action on systemic blood pressure, heart rate and coronary, carotid, vertebral, renal, and mesenteric blood flows. It is the only clinical compound with this profile. It is currently being investigated in the treatment of peripheral vascular diseases and Raynaud's syndrome.
Drug Indication Investigated for use/treatment in peripheral vascular disease and raynaud's disease. Mechanism of Action At low doses, OPC 28326 selectively vasodilates the femoral arterial bed due to its inhibitory action at alpha-2C-adrenoceptors. Other studies have also reported selectivity for a-2B-adrenoceptors. Pharmacodynamics At low doses, OPC 28326 selectively vasodilates the femoral arterial bed due to its inhibitory action at alpha-2-adrenoceptors while having minimal action on systemic blood pressure, heart rate and coronary, carotid, vertebral, renal, and mesenteric blood flows. |
| Molecular Formula |
C26H38CLN3O3
|
|---|---|
| Molecular Weight |
476.0512
|
| Exact Mass |
421.272
|
| CAS # |
167626-17-7
|
| Related CAS # |
478946-89-3 (OPC-28326 free);
|
| PubChem CID |
219020
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.1±0.1 g/cm3
|
| Boiling Point |
624.5±55.0 °C at 760 mmHg
|
| Flash Point |
331.5±31.5 °C
|
| Vapour Pressure |
0.0±1.8 mmHg at 25°C
|
| Index of Refraction |
1.590
|
| LogP |
3.59
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
31
|
| Complexity |
569
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
Cl[H].O=C(C1C([H])=C(C([H])([H])[H])C(=C(C([H])([H])[H])C=1[H])N([H])C(C([H])([H])C([H])([H])[H])=O)N1C([H])([H])C([H])([H])C([H])(C([H])([H])C1([H])[H])N(C([H])([H])[H])C([H])([H])C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H].O([H])[H]
|
| InChi Key |
BESKMDLUOAVUJF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C26H35N3O2/c1-5-24(30)27-25-19(2)17-22(18-20(25)3)26(31)29-15-12-23(13-16-29)28(4)14-11-21-9-7-6-8-10-21/h6-10,17-18,23H,5,11-16H2,1-4H3,(H,27,30)
|
| Chemical Name |
N-[2,6-dimethyl-4-[4-[methyl(2-phenylethyl)amino]piperidine-1-carbonyl]phenyl]propanamide
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.1006 mL | 10.5031 mL | 21.0062 mL | |
| 5 mM | 0.4201 mL | 2.1006 mL | 4.2012 mL | |
| 10 mM | 0.2101 mL | 1.0503 mL | 2.1006 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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