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- 上海莼试
- CS-01Y76734
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- 2025年07月14日
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- 详细信息
- 技术资料
- 库存：
23
- 英文名：
Olcegepant
- CAS号：
204697-65-4
- 供应商：
上海莼试
- 保存条件：
Store at -20°C
- 规格：
10mg 5mg 50mg 1g
产品描述：
分子式:C38H47Br2N9O5
分子量:869.66
溶解度:≥ 87 mg/mL in DMSO with gentle warming
储存条件:Store at -20°C
General tips:For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition:Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
Olcegepant Description:IC50: 0.1nM on human brain vessels [1]Olcegepant is the first potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor, a key modulator in neurogenic inflammatory pain. Under development by Boehringer Ingelheim GmbH, olcegepant is an intravenously formulated treatment for acute attacks of migraine.In vitro: Functional studies with SK-N-MC cells demonstrated that CGRP-induced cAMP production was antagonised by both CGRP- (8-37) and olcegepant with pA2 values of 7.8 and 11.2, respectively. [1].In vivo: Pre-treatment with olcegepant (900 mg/kg) inhibited the capsaicin-induced expression of Fos throughout the spinal trigeminal nucleus by 57%. In contrast, the expression of phosphorylated extracellular signal-regulated kinase in the trigeminal ganglion was not changed by olcegepant pre-treatment. CGRP receptor inhibition, which has been shown to decrease spinal trigeminal activity, is likely to occur in the central nervous system rather than in the periphery including the trigeminal ganglion. This may be important for future therapeutic interventions with CGRP receptor antagonists in migraine. [2].Clinical trial: In a phase II clinical trial, olcegepant reduced the severity of headache in 60% of migraine sufferers and met secondary endpoints including headache-free rate and rate of sustained response. Only mild-to-moderate transient adverse events were orved, with no adverse cardiovascular symptoms reported. The compound appears to be an effective anti-migraine medication that is well tolerated and does not display the vasoconstrictive effect that precludes the use of triptans and dihydroergotamin in certain patients [3].
商品属性：
注意事项：
抗逆滴加序列
每次向板内滴加抗原时，移液器滴头要与平面45度悬空，不要触碰到孔内的液体，由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下，必须反应30min以上，若环境温度低于室温，可将微量反应板置于恒温培养箱中，使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定，往往在高压后pH值会有所改变，所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时，红细胞会产生自凝现象;当pH>7.8时，图形洗脱加快，易造成肉眼观察产生误差;p H=7.2时，红细胞沉降最充分，图形最清晰。
当滴注 1%红细胞悬液时，应经常摇晃红细胞悬液，使红细胞均匀地分布在磷酸缓冲液中，以防止红细胞下降。
反应时间及温度
加入鸡红血球之后，反应板在室温(20~25℃)静置30~40min，对照孔血球下沉于孔底，即可判定结果。若室温达不到实验要求，需相应调整反应时间。当环境温度低于4℃时，红细胞发生自凝;高于37℃时，会发生反应物分离和红细胞溶血。
公司正在出售的产品：
使用方法：
1.本蛋白酶抑制剂混合物为100×的储存液，使用时按照1:100的比例加入到裂解液中(例如，1ml裂解液中加入10μl蛋白酶抑制剂混合物)，混匀后即可使用。根据需要，0.5M的EDTA也按照1:100的比例加入到裂解液中（如用于检测金属蛋白酶活性，则不宜添加EDTA）。含有蛋白酶抑制剂混合物的裂解液宜现用现配，不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后，就可以开始进行哺乳动物组织的裂解和蛋白提取。
分子式:C38H47Br2N9O5
分子量:869.66
溶解度:≥ 87 mg/mL in DMSO with gentle warming
储存条件:Store at -20°C
General tips:For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition:Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
Olcegepant Description:IC50: 0.1nM on human brain vessels [1]Olcegepant is the first potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor, a key modulator in neurogenic inflammatory pain. Under development by Boehringer Ingelheim GmbH, olcegepant is an intravenously formulated treatment for acute attacks of migraine.In vitro: Functional studies with SK-N-MC cells demonstrated that CGRP-induced cAMP production was antagonised by both CGRP- (8-37) and olcegepant with pA2 values of 7.8 and 11.2, respectively. [1].In vivo: Pre-treatment with olcegepant (900 mg/kg) inhibited the capsaicin-induced expression of Fos throughout the spinal trigeminal nucleus by 57%. In contrast, the expression of phosphorylated extracellular signal-regulated kinase in the trigeminal ganglion was not changed by olcegepant pre-treatment. CGRP receptor inhibition, which has been shown to decrease spinal trigeminal activity, is likely to occur in the central nervous system rather than in the periphery including the trigeminal ganglion. This may be important for future therapeutic interventions with CGRP receptor antagonists in migraine. [2].Clinical trial: In a phase II clinical trial, olcegepant reduced the severity of headache in 60% of migraine sufferers and met secondary endpoints including headache-free rate and rate of sustained response. Only mild-to-moderate transient adverse events were orved, with no adverse cardiovascular symptoms reported. The compound appears to be an effective anti-migraine medication that is well tolerated and does not display the vasoconstrictive effect that precludes the use of triptans and dihydroergotamin in certain patients [3].
商品属性：
| 货号 | CS-01Y76734 | 规格 | 10mg 5mg 50mg 1g |
| CAS号 | 204697-65-4 | 分子量 | 869.66 |
| 含量 | >99.50% | 别名 | BIBN-4096; BIBN-4096BS;BIBN4096BS; BIBN 4096BS |
| 分子式 | C38H47Br2N9O5 | 化学名 | |
| 产地 | 国产 | 用途 | 仅供科研研究实验 |
抗逆滴加序列
每次向板内滴加抗原时，移液器滴头要与平面45度悬空，不要触碰到孔内的液体，由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下，必须反应30min以上，若环境温度低于室温，可将微量反应板置于恒温培养箱中，使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定，往往在高压后pH值会有所改变，所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时，红细胞会产生自凝现象;当pH>7.8时，图形洗脱加快，易造成肉眼观察产生误差;p H=7.2时，红细胞沉降最充分，图形最清晰。
当滴注 1%红细胞悬液时，应经常摇晃红细胞悬液，使红细胞均匀地分布在磷酸缓冲液中，以防止红细胞下降。
反应时间及温度
加入鸡红血球之后，反应板在室温(20~25℃)静置30~40min，对照孔血球下沉于孔底，即可判定结果。若室温达不到实验要求，需相应调整反应时间。当环境温度低于4℃时，红细胞发生自凝;高于37℃时，会发生反应物分离和红细胞溶血。
公司正在出售的产品：
| Boc-D-Glu(OFm)-OH | PPADS tetrasodium salt |
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| PPARα-MO-1 | 胃抑素检测试剂盒 GIP ELISA Kit |
| Pparδ agonist | 胃泌素细胞抗检测试剂盒 GCA ELISA Kit |
| Pparδ agonist 1 | 胃内因子检测试剂盒 GIF ELISA Kit |
| Pparδ agonist 2 | 胃泌素释放肽前检测试剂盒 ProGRP ELISA Kit |
| PPDA | 胃泌素释放多肽检测试剂盒 GRP ELISA Kit |
| PPNDS | MMP-3 ELISA Kit |
| PPOH | 胃粘液素检测试剂盒 GM ELISA Kit |
| PPPA | 蜗同源物2检测试剂盒 SNAI2 ELISA Kit |
| PPQ-102 | 乌头酸酶2检测试剂盒 ACO-2 ELISA Kit |
| PPT | 无花果酶2检测试剂盒 FCN2 ELISA Kit |
| PPY A | Olcegepant舞蹈病蛋白相互作用蛋白1检测试剂盒 HIP1 ELISA Kit |
| CETP-IN-3 | 戊型肝炎IgG检测试剂盒 HEV-IgG ELISA Kit |
| 硒蛋白S检测试剂盒 SELS ELISA Kit | 戊型肝炎IgM检测试剂盒 HEV-IgM ELISA Kit |
1.本蛋白酶抑制剂混合物为100×的储存液，使用时按照1:100的比例加入到裂解液中(例如，1ml裂解液中加入10μl蛋白酶抑制剂混合物)，混匀后即可使用。根据需要，0.5M的EDTA也按照1:100的比例加入到裂解液中（如用于检测金属蛋白酶活性，则不宜添加EDTA）。含有蛋白酶抑制剂混合物的裂解液宜现用现配，不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后，就可以开始进行哺乳动物组织的裂解和蛋白提取。
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Olcegepant
￥600 - 3200
