| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vivo |
In a dose-dependent manner, NKH477 (Colforsin dapropate hydrochloride) (oral; 1-3 mg/kg/day; days 3 and 5) improves lung allograft survival [1].
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|---|---|
| Animal Protocol |
Animal/Disease Models: Specific pathogen-free inbred male Lewis rat (LEW), weighing 250 to 280 g [1]
Doses: 1, 2 or 3 mg/kg/day Doses: Oral; daily; day 3 and Day 5 Experimental Results: Lung allograft survival was dose-dependently prolonged. |
| References | |
| Additional Infomation |
Colforsin daropate hydrochloride is the hydrochloride salt of colforsin daropate. It is a drug used for the treatment of acute heart failure. It directly stimulates adenylate cyclase and produces positive inotropic and vasodilator effects accompanied by the increase in cellular cAMP. It has a role as an adenylate cyclase agonist, an antihypertensive agent, a cardiotonic drug and a vasodilator agent. It contains a colforsin daropate(1+).
Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant Coleus forskohlii. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland. |
| Molecular Formula |
C28H45CLO8
|
|---|---|
| Molecular Weight |
545.11
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| Exact Mass |
545.275
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| CAS # |
138605-00-2
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| PubChem CID |
444028
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| Appearance |
White to off-white solid powder
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| Boiling Point |
571.4ºC at 760mmHg
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| Flash Point |
176ºC
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| Vapour Pressure |
5.29E-16mmHg at 25°C
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| LogP |
2.824
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
37
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| Complexity |
933
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| Defined Atom Stereocenter Count |
8
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| SMILES |
C=C[C@@]1(C)CC(=O)[C@@]2([C@@]3(C)[C@H](CCC(C)(C)[C@@H]3[C@@H]([C@@H]([C@@]2(C)O1)OC(=O)C)OC(=O)CCN(C)C)O)O.Cl
|
| InChi Key |
LNEICJSEZPSKSJ-RPBMHHKSSA-N
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| InChi Code |
InChI=1S/C28H44O8.ClH/c1-10-25(7)15-19(31)28(33)26(8)18(30)13-14-24(5,6)22(26)21(35-20(32)12-11-16(2)3)23(34-17(4)29)27(28,9)36-25/h10,16,18,21-23,30,33H,1,11-15H2,2-9H31H/t18-,21-,22-,23-,25-,26-,27+,28-/m0./s1
|
| Chemical Name |
(3R,4aR,5S,6S,6aS,10S,10aR,10bS)-5-(acetyloxy)-3-ethenyl-10,10b-dihydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-dodecahydro-1H-naphtho[2,1-b]pyran-6-yl 4-methylpentanoate hydrochloride
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| Synonyms |
NKH 477 NKH-477 NKH477
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. (3). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| 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 : ~125 mg/mL (~228.90 mM)
H2O : ~20 mg/mL (~36.62 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.81 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8345 mL | 9.1725 mL | 18.3449 mL | |
| 5 mM | 0.3669 mL | 1.8345 mL | 3.6690 mL | |
| 10 mM | 0.1834 mL | 0.9172 mL | 1.8345 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00864578 | WITHDRAWN | Intraocular Pressure Primary Open Angle Glaucoma |
Sooft Italia | 2009-04 | ||
| NCT02143349 | UNKNOWN STATUS | Dietary Supplement: Coleus forskohlii extract
Other: Placebo |
Metabolic Syndrome Obesity |
Olive Lifesciences Pvt Ltd | 2014-04 | Phase 3 |
| NCT03652090 | COMPLETED | Procedure: cell sampling | Cystic Fibrosis | Institut National de la Santé Et de la Recherche Médicale, France | 2010-09-01 | |
| NCT04254705 | WITHDRAWN | Procedure: Rectal Biopsy | Cystic Fibrosis | Universitaire Ziekenhuizen KU Leuven | 2020-03-01 | Not Applicable |
| NCT01254006 | COMPLETED | Drug: forskolin, rutin and vitamins B1 and B2 | Glaucoma | University of Roma La Sapienza | Not Applicable |
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