| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
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| 100mg |
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| Other Sizes |
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| References | |
|---|---|
| Additional Infomation |
Revaprazan Hydrochloride is the hydrochloride salt form of a lipophilic, weak base with potassium-competitive acid blocking (P-CAB) activity. Revaprazan concentrates highly in the gastric parietal cell canaliculus and on entering this acidic environment is instantly protonated and binds competitively and reversibly to the potassium binding site of the proton pump hydrogen-potassium adenosine triphosphatase (H+/K+ ATPase), thereby inhibiting the pump's activity and the parietal cell secretion of H+ ions into the gastric lumen, the final step in gastric acid production.
See also: Revaprazan (annotation moved to). |
| Exact Mass |
398.167
|
|---|---|
| CAS # |
178307-42-1
|
| Related CAS # |
199463-33-7;178307-42-1 (HCl);
|
| PubChem CID |
204103
|
| Appearance |
White to off-white solid powder
|
| Melting Point |
205-208°
|
| LogP |
6.039
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
28
|
| Complexity |
481
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1=C(C)N=C(NC2=CC=C(C=C2)F)N=C1N3CCC4=CC=CC=C4C3C.Cl
|
| InChi Key |
MALPZYQJEDBIAK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H23FN4.ClH/c1-14-15(2)24-22(25-19-10-8-18(23)9-11-19)26-21(14)27-13-12-17-6-4-5-7-20(17)16(27)3;/h4-11,16H,12-13H2,1-3H3,(H,24,25,26);1H
|
| Chemical Name |
N-(4-fluorophenyl)-4,5-dimethyl-6-(1-methyl-3,4-dihydro-1H-isoquinolin-2-yl)pyrimidin-2-amine;hydrochloride
|
| Synonyms |
YH 1885 YH-1885Revaprazan Hydrochloride YH1885
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~8.33 mg/mL (~20.88 mM)
H2O : < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.56 mg/mL (3.91 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 15.6 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: ≥ 1.56 mg/mL (3.91 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 15.6 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: ≥ 1.56 mg/mL (3.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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 |
| NCT01332890 | COMPLETED | Other: Sequence 1 Other: Sequence 2 Other: Sequence 3 |
Healthy | Yuhan Corporation | 2011-04 | Phase 1 |
| NCT03378284 | COMPLETED | Drug: Tegoprazan Drug: Revaprazan |
Healthy Male Volunteers Pharmacodynamics |
HK inno.N Corporation | 2017-12-10 | Phase 1 |
| NCT01750437 | COMPLETED | Drug: YH1885L(Revaprazan) Drug: Esomeprazole 20mg Drug: placebo |
Non-erosive Reflux Disease | Yuhan Corporation | 2013-01 | Phase 2 |
Products are for research use only; We do not sell to patients
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