Revaprazan hydrochloride
(Synonyms: 盐酸瑞伐拉赞) 目录号 : GC38198
Revaprazan Hydrochloride (YH1885) is a new reversible proton pump inhibitor with long-lasting acid-suppressive effects. Revaprazan Hydrochloride reversibly inhibits H(+)/K(+)-ATPase via binding to the K+-binding site of the pump.
Cas No.:178307-42-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Revaprazan Hydrochloride (YH1885) is a new reversible proton pump inhibitor with long-lasting acid-suppressive effects. Revaprazan Hydrochloride reversibly inhibits H(+)/K(+)-ATPase via binding to the K+-binding site of the pump.
Revaprazan Hydrochloride reversibly inhibits H+/K+-ATPase via binding to the K+-binding site of the pump. This reversibility leads to fewer adverse events[1]. Revaprazan could inhibit H.pylori-induced COX-2 expression by blocking phosphorylation of IκB-α and Akt signaling in AGS cells. It could impose significant anti-inflammatory actions on H.pylori infection beyond acid suppression[2].
Pharmacokinetic studies of revaprazan hydrochloride in rats and dogs showed the drug had a low oral bioavailability, which was speculated to be due to first pass effect and poor water solubility of drug[1].
[1] Li W, et al. Int J Pharm. 2011, 408(1-2):157-62. [2] Lee JS, et al. J Clin Biochem Nutr. 2012, 51(2):77-83.
| Cas No. | 178307-42-1 | SDF | |
| 别名 | 盐酸瑞伐拉赞 | ||
| Canonical SMILES | CC1=C(C)C(N2C(C)C3=C(C=CC=C3)CC2)=NC(NC4=CC=C(F)C=C4)=N1.[H]Cl | ||
| 分子式 | C22H24ClFN4 | 分子量 | 398.9 |
| 溶解度 | DMSO: 8.33 mg/mL (20.88 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5069 mL | 12.5345 mL | 25.0689 mL |
| 5 mM | 0.5014 mL | 2.5069 mL | 5.0138 mL |
| 10 mM | 0.2507 mL | 1.2534 mL | 2.5069 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Preparation and in vitro/in vivo evaluation of Revaprazan hydrochloride nanosuspension
Int J Pharm 2011 Apr 15;408(1-2):157-62.PMID:21295124DOI:10.1016/j.ijpharm.2011.01.059.
Revaprazan hydrochloride (RH) is a new reversible proton pump inhibitor. However, due to poor water solubility, oral bioavailability of the drug was relatively low. To investigate the particle size reduction effect of RH on dissolution and absorption, three suspensions that containing different sized particles were prepared by high pressure homogenization and in vitro/in vivo evaluations were carried out. DSC and powder X-ray diffraction were used to study crystalline state of freeze dried powder of RH suspensions and the results showed that particles of RH microsuspension and nanosuspension remained in the same crystalline state as coarse suspension, but had lower lattice energy. In the in vitro dissolution test, both microsuspension and nanosuspension showed increased dissolution rate. In the in vivo evaluation, compared to coarse suspension, RH nanosuspension exhibited significant increase in AUC(0-t), C(max) and decrease in T(max), MRT. Nevertheless, RH microsuspension did not display any significant differences in these pharmacokinetic parameters compared to the coarse suspension. The findings revealed that particle size reduction can influence RH absorption in gastrointestinal tract and nanosuspension can enhance oral bioavailability of RH in rats.
Comparison of a revaprazan-loaded solid dispersion, solid SNEDDS and inclusion compound: Physicochemical characterisation and pharmacokinetics
Colloids Surf B Biointerfaces 2018 Feb 1;162:420-426.PMID:29248606DOI:10.1016/j.colsurfb.2017.12.017.
The aim of this research was to compare three strategies for enhancing the solubility of poorly water-soluble Revaprazan hydrochloride: solid dispersion, solid SNEDDS and inclusion compound. The influence of polymers, surfactants and oils on the drug solubility was assessed, and via the chosen carriers, the three types of formulations were prepared utilising spray drying technique. Their physicochemical properties, solubility, dissolution and pharmacokinetics in rats were performed compared with revaprazan powder. Among the liquid SNEDDS formulations assessed, the compositions of revaprazan, peceol, Tween 80 and Labrasol (10:15:55:30, weight ratio) provided the smallest emulsion size. Moreover, this liquid SNEDDS and dextran were suspended/dissolved in distilled water, and spray-dried, producing an optimal revaprazan-loaded solid SNEDDS. The appropriate solid dispersion and inclusion compound were composed of revaprazan, hydroxypropylmethylcellulose and cremophor A25 (5:1.4:5.6) and drug and hydroxyl-β-cyclodextrin (2.5:8.77), respectively. The crystalline drug was converted to an amorphous state in all formulations. In the solid dispersion, the drug was attached to the hydrophilic carrier. The solid SNEDDS and inclusion compound contained aggregate microspheres and separate microspheres, respectively. All formulations significantly increased the drug solubility, dissolution, plasma concentration and AUC compared with revaprazan powder. These properties were ranked in the order solid dispersion ≥ solid SNEDDS > inclusion compound. Particularly, the solid dispersion improved about 9500-fold drug solubility and 10-fold oral bioavailability. Thus, the improved properties were considerably dependent upon these techniques, although all of the techniques employed similar mechanisms. Among the strategies checked, the solid dispersion system would be recommended as an oral revaprazan-loaded pharmaceutical product.
Gateways to clinical trials
Methods Find Exp Clin Pharmacol 2007 Mar;29(2):153-73.PMID:17440629doi
Agomelatine, AGRO-100, AIDSVAX gp120 B/E, alfimeprase, aliskiren fumarate, ALVAC vCP1452, alvocidib hydrochloride, ambrisentan, AME-527, AN-0128, apadenoson, ARRY-142886, asenapine maleate, axitinib, azimilide hydrochloride; Belimumab, bevacizumab, biolimus A9, BiovaxID, bryostatin 1; Cannabidiol, celgosivir, CG-1940/CG-8711, CKD-501, collagen-PVP, CpG-10101, CTL-102, CTL-102/CB-1954; D-4F, darusentan, dexverapamil, DNA influenza vaccine, dronabinol/cannabidiol, dronedarone hydrochloride; Eculizumab, edodekin alfa, edotecarin, enzastaurin hydrochloride; Fingolimod hydrochloride; Golimumab; HBV-DNA vaccine, hyaluronic acid; I-131 ch-TNT-1/B, imatinib mesylate, inhaled insulin, ipilimumab, ispinesib mesylate, i.v. gamma-globulin; KU-59436; Lapaquistat; Mapatumumab, MC-1, MC-1/lisinopril, mepolizumab; Nibentan, nilotinib, Nobori, NV1FGF; Ocrelizumab; Paclimer, pagoclone, paliperidone, PC-515, PHA-794428, phosphostim, PPI-2458, prasugrel, PTC-299; Renzapride hydrochloride, Reolysin, reslizumab, Revaprazan hydrochloride, rivaroxaban, romidepsin, rubitecan, ruboxistaurin mesilate hydrate; Sapacitabine, SarCNU, ST-1859, sunitinib malate; Tanespimycin, temsirolimus, tgAAC-94, TGN-255, ticagrelor, tipifarnib, tolvaptan, tretazicar, TRU-015; Upgrade varicella vaccine, Ushercell; Vernakalant hydrochloride, verpasep caltespen, VNP-40101M, VRC-HIVADV014-00-VP, VRC-HIVDNA009-00-VP, VX-001; XL-647, XL-820, XL-880, XL-999.
Gateways to clinical trials
Methods Find Exp Clin Pharmacol 2009 Apr;31(3):183-226.PMID:19536362doi
(+)-Dapoxetine hydrochloride, [(123)I]-BZA, 9-Aminocamptothecin; Abacavir sulfate/lamivudine, Adalimumab, Adefovir dipivoxil, Alemtuzumab, Alvocidib hydrochloride, Ambrisentan, Amsilarotene, Anacetrapib, Anakinra, Apricitabine, Aripiprazole, Arsenic trioxide, Atazanavir sulfate, Atazanavir/ritonavir, Atrasentan, Azacitidine; Banoxantrone, Bazedoxifene acetate, Bevacizumab, Bexarotene, Biphasic insulin aspart, Bortezomib, Bosentan, Bromfenac; Cachectin, Calcipotriol/betamethasone dipropionate, Canakinumab, Carfilzomib, CAT-354, CCX-282, Certolizumab pegol, Cetuximab, Choline fenofibrate, Clevudine, Clofarabine, CNTO-328, Corifollitropin alfa, Crofelemer; Daptomycin, Darbepoetin alfa, Darunavir, Dasatinib, Decitabine, Deferasirox, Denosumab, Duloxetine hydrochloride, Dutasteride; Emtricitabine, Enfuvirtide, Entecavir, Epoetin zeta, Erlotinib hydrochloride, Escitalopram oxalate, Eslicarbazepine acetate, Eszopiclone, Etravirine, Everolimus, Exenatide, Ezetimibe, Ezetimibe/simvastatin; Farglitazar, Febuxostat, Fosamprenavir calcium, FX-06; Gabapentin enacarbil, Gefitinib; HIVIS DNA; Imatinib mesylate, INCB- 18424, Indacaterol, Inotuzumab ozogamicin, Insulin detemir; JNJ-26854165; Lacosamide, Landiolol, Laromustine, Lenalidomide, Liposomal doxorubicin, L-NAME, Lopinavir, Lopinavir/ritonavir, Lumiracoxib; Maraviroc, Mepolizumab, Methoxy polyethylene glycol- epoetin-beta, Miglustat, MK-0493, MVA-CMDR, Mycophenolic acid sodium salt; Natalizumab, Nepafenac, Neratinib, Neridronic acid, Nesiritide, Nilotinib hydrochloride monohydrate; Olmesartan medoxomil, Omacetaxine mepesuccinate, Omalizumab; Paclitaxel poliglumex, Palifermin, Patupilone, Pegfilgrastim, Peginterferon alfa-2a, Peginterferon alfa-2b, Peginterferon alfa-2b/ ribavirin, Pemetrexed disodium, PHA-848125, Pitavastatin calcium, Posaconazole, Povidone-iodine liposome complex, Prasugrel, Pregabalin, Prucalopride; Raltegravir potassium, Retigabine, Revaprazan hydrochloride, rhFSH, Rilpivirine, Rivaroxaban, Romidepsin, Rosuvastatin calcium, RWJ-676070; SAR-109659, Sitagliptin phosphate monohydrate, Sorafenib, Stavudine/Lamivudine/Nevirapine, Sunitinib malate; Tadalafil, Telaprevir, Telbivudine, Tenofovir disoproxil fumarate, Tenofovir disoproxil fumarate/emtricitabine, Tenofovir disoproxil fumarate/emtricitabine/efavirenz, Teriparatide, Tigecycline, Tiotropium bromide, Tipifarnib, Tipranavir, Tocilizumab, Trifluridine/TPI; UP-780; Vandetanib, Vardenafil hydrochloride hydrate, Vatalanib succinate, Vitespen, Vorinostat; Yttrium 90 (90Y) ibritumomab tiuxetan; Zoledronic acid monohydrate.