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131543-23-2

中文名稱(chēng) (R)-(+)-WIN 55,212-2 甲磺酸鹽
英文名稱(chēng) WIN 55,212-2 MESYLATE
CAS 131543-23-2
分子式 C28H30N2O6S
分子量 522.61
MOL 文件 131543-23-2.mol
更新日期 2024/12/20 11:58:07
131543-23-2 結(jié)構(gòu)式 131543-23-2 結(jié)構(gòu)式

基本信息

中文別名
水溶性西地那非
甲磺酸西地那非(Z)
WIN552122 甲磺酸酯
甲磺酸西地那非(酒溶西地那非)
WIN 55212-2 甲磺酸鹽
(+)WIN 55212-2甲磺酸鹽
化合物WIN 55,212-2 MESYLATE
(R)-(+)-WIN 55,212-2 甲磺酸鹽
(+)-WIN 55,212-2 (MESYLATE)
WIN552122 甲磺酸酯 WIN552122 MESYLATE
英文別名
WIN55
CS-754
WIN 55,212-2
212-2Mesylate
WIN552122
WIN-552122
WIN 55,212-2 MESYLATE
R(+)-WIN 55,212-2 MESYLATE
WIN 55212-2 methanesulfonate
(R)-(+)-WIN 55,212-2 mesylate salt
WIN552122
WIN-552122
(R)-(+)-WIN 55212
所屬類(lèi)別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

儲(chǔ)存條件Store at +4°C
溶解度0.1 M HCl: 0.25 mg/mL
溶解度0.1 M HCl:0.25 mg/mL
形態(tài)solid
顏色white to off-white
穩(wěn)定性DMSO中的溶液可在-20°下穩(wěn)定儲(chǔ)存3個(gè)月。
InChIKeyFSGCSTPOPBJYSX-OZYVVJTJNA-N
SMILESS(O)(=O)(=O)C.C(N1CCOCC1)[C@@H]1COC2=CC=CC3C(C(C4=CC=CC5=CC=CC=C45)=O)=C(C)N1C=32 |&1:12,r|

安全數(shù)據(jù)

WGK Germany3
WGK Germany3

常見(jiàn)問(wèn)題列表

概述
(R)-(+)-WIN 55,212-2 甲磺酸鹽是生產(chǎn)西地那非的原料, 西地那非俗稱(chēng)偉哥,因治療男性勃起功能障礙(ED)而聞名,其實(shí)最早是一種為治療心血管疾病而研發(fā)的藥物。目前不僅驗(yàn)證了西地那非對(duì)ED的治療作用,而且也證明了西地那非對(duì)肺動(dòng)脈高壓等疾病也有治療作用。西地那非通過(guò)抑制磷酸二酯酶5(PDE5),增加陰莖海綿體內(nèi)環(huán)磷酸鳥(niǎo)苷(cGMP)水平,松弛海綿體平滑肌,血液流入海綿體,改善性刺激引起的勃起反應(yīng),藥效可持續(xù)4小時(shí)。
生物活性
WIN 55,212-2 Mesylate ((R)-(+)-WIN 55212)是一種有效的 cannabinoid (CB) receptor 的激動(dòng)劑,對(duì)人重組CB2和CB1的Ki值分別為3.3 nM和62.3 nM。 WIN 55,212-2 Mesylate 可調(diào)節(jié)谷氨酸的傳遞。
靶點(diǎn)
TargetValue
CB2
(Cell-free assay)
3.3 nM(Ki)
CB1
(Cell-free assay)
62.3 nM(Ki)
體外研究

WIN 55,212-2 is more potent in CHO-CB2 cells than in CHO-CB1 cells by a factor of 6O. WIN 55,212-2 has no effect on arachidonic acid release in CHO-CB2 or control CHO cells. WIN 55,212-2 fails to stimulate any increase in intracellular Ca 2+ up to 10 μM. In primary cultures of rat cerebral cortex neurons, WIN 55,212-2 (0.01--100 nM) increases extracellular glutamate levels, displaying a bell-shaped concentration-response curve. The facilitatory effect of WIN 55,212-2 (1 nM) is fully counteracted by SR141716A (10 nM), by the replacement of the normal Krebs Ringer-bicarbonate buffer with a low Ca 2+ medium (0.2 mM) and by the IP(3) receptor antagonist xestospongin C (1 μM). WIN 55,212-2 evokes CGRP release from TG neurons in vitro (EC 50 =26 μM) in a concentration- and calcium-dependent manner. WIN 55,212-2-2 neither inhibits capsaicin-evokes CGRP release nor does it inhibit forskolin-, isoproteranol- or prostaglandin E2-stimulated cAMP accumulation. WIN 55,212-2 significantly inhibits (EC 50 =1.7 μM) 50 mm K + -evoked CGRP release by approximately 70%. WIN 55,212-2 inhibition of 50 mm K + -evoked CGRP release is not reversed by antagonists of cannabinoid type 1 (CB1) receptor, but is mimicks in magnitude and potency (EC 50 =2.7 μM) by its cannabinoid-inactive enantiomer WIN 55,212-2-3.

體內(nèi)研究

In the prefrontal cortex WIN 55,212-2 (0.1 and 1 mg/kg i.p.) increases dialysate glutamate levels from of the awake rat, while the lower (0.01 mg/kg) and the higher (2 mg/kg) doses are ineffective. Furthermore, the WIN 55,212-2 (0.1 mg/kg)- induced increase of dialysate glutamate levels is counteracted by pretreatment with the selective CB(1) receptor antagonist SR141716A (0.1 mg/kg, i.p.) and by the local perfusion with a low-calcium Ringer solution (Ca 2+ 0.2 mM). WIN 55,212-2 (0.5, 1, 3, 5, 10 and 15 mg/kg, i.p.) does not alter the seizure threshold at low doses, while higher doses of the drug significantly increases the threshold in a dose-dependent manner. The anticonvulsant effect of WIN 55,212-2, which is observed with doses as high as 5 mg/kg, can be observed with doses as low as 0.5 mg/kg in groups pre-treated with 20 mg/kg of pioglitazone.

(R)-(+)-WIN 55,212-2 甲磺酸鹽價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱(chēng)CAS號(hào)包裝價(jià)格
2024/11/08W0019WIN 55212-2甲磺酸鹽
WIN 55212-2 Mesylate
131543-23-250MG1290元
2023/03/20HY-13291(R)-(+)-WIN 55,212-2 甲磺酸鹽
WIN 55,212-2 Mesylate
131543-23-25mg810元
2023/03/20HY-13291(R)-(+)-WIN 55,212-2 甲磺酸鹽
WIN 55,212-2 Mesylate
131543-23-210mg1350元
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