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My CartCAS：9087-70-1
Storage：Powder:-20℃，1 year;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 9087-70-1 |
| Name | Aprotinin |
| Molecular Formula | C284H432N84O79S7 |
| Molecular Weight | 6511.44 |
| Solubility | Soluble in Water ≥20mg/mL |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:-20℃，1 year;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 232-994-9 |
| MDL | MFCD00130541 |
| SMILES | [RPDFCLEPPYTGPCKARIIRYFYNAKAGLCQTFVYGGCRAKRNNFKSAEDCMRTCGGA] |
| InChIKey | ZPNFWUPYTFPOJU-UHFFFAOYSA-N |
| InChI | InChI=1S/C284H432N84O79S7/c1-21-144(9)222-271(439)337-174(68-46-105-309-282(300)301)239(407)340-187(120-160-77-85-164(374)86-78-160)251(419)341-185(116-156-55-29-24-30-56-156)250(418)342-188(121-161-79-87-165(375)88-80-161)252(420)346-191(123-208(291)378)246(414)322-149(14)230(398)326-168(62-35-39-98-285)234(402)319-146(11)227(395)314-132-215(385)324-181(113-141(3)4)247(415)354-199-137-452-453-138-200-263(431)336-179(97-112-448-20)242(410)331-176(70-48-107-311-284(304)305)244(412)363-226(154(19)372)274(442)358-197(233(401)316-129-212(382)312-130-213(383)318-151(16)278(446)447)135-449-451-139-201(355-253(421)186(117-157-57-31-25-32-58-157)344-256(424)195(127-220(393)394)350-267(435)204-72-50-109-366(204)275(443)167(289)61-43-102-306-279(294)295)265(433)339-182(114-142(5)6)248(416)338-180(93-96-218(389)390)276(444)368-111-52-74-206(368)277(445)367-110-51-73-205(367)268(436)349-189(122-162-81-89-166(376)90-82-162)259(427)362-224(152(17)370)269(437)317-133-216(386)365-108-49-71-203(365)266(434)357-202(264(432)333-169(63-36-40-99-286)235(403)320-148(13)229(397)328-175(69-47-106-310-283(302)303)243(411)360-223(145(10)22-2)272(440)361-222)140-454-450-136-198(325-214(384)131-313-211(381)128-315-232(400)183(119-159-75-83-163(373)84-76-159)351-270(438)221(143(7)8)359-258(426)190(118-158-59-33-26-34-60-158)352-273(441)225(153(18)371)364-245(413)177(335-262(199)430)91-94-207(290)377)261(429)334-172(66-44-103-307-280(296)297)236(404)321-147(12)228(396)327-170(64-37-41-100-287)237(405)330-173(67-45-104-308-281(298)299)238(406)345-192(124-209(292)379)255(423)347-193(125-210(293)380)254(422)343-184(115-155-53-27-23-28-54-155)249(417)332-171(65-38-42-101-288)240(408)353-196(134-369)260(428)323-150(15)231(399)329-178(92-95-217(387)388)241(409)348-194(126-219(391)392)257(425)356-200/h23-34,53-60,75-90,141-154,167-206,221-226,369-376H,21-22,35-52,61-74,91-140,285-289H2,1-20H3,(H2,290,377)(H2,291,378)(H2,292,379)(H2,293,380)(H,312,382)(H,313,381)(H,314,395)(H,315,400)(H,316,401)(H,317,437)(H,318,383)(H,319,402)(H,320,403)(H,321,404)(H,322,414)(H,323,428)(H,324,385)(H,325,384)(H,326,398)(H,327,396)(H,328,397)(H,329,399)(H,330,405)(H,331,410)(H,332,417)(H,333,432)(H,334,429)(H,335,430)(H,336,431)(H,337,439)(H,338,416)(H,339,433)(H,340,407)(H,341,419)(H,342,418)(H,343,422)(H,344,424)(H,345,406)(H,346,420)(H,347,423)(H,348,409)(H,349,436)(H,350,435)(H,351,438)(H,352,441)(H,353,408)(H,354,415)(H,355,421)(H,356,425)(H,357,434)(H,358,442)(H,359,426)(H,360,411)(H,361,440)(H,362,427)(H,363,412)(H,364,413)(H,387,388)(H,389,390)(H,391,392)(H,393,394)(H,446,447)(H4,294,295,306)(H4,296,297,307)(H4,298,299,308)(H4,300,301,309)(H4,302,303,310)(H4,304,305,311) |
| PubChem CID | 22833874 |
| Target Point | Serine Protease |
| Passage | Metabolic Enzyme&Protease |
| Background | Aprotinin is a serine protease (BPTI) inhibitor. |
| Biological Activity | Aprotinin是丝氨酸蛋白酶 (BPTI) 抑制剂，对胰蛋白酶和胰凝乳蛋白酶胰凝乳蛋白酶的 Ki 值分别为0.06 pM和9 nM。[1-6] |
| In Vitro | 抑肽酶是一种从牛肺中分离出的丝氨酸蛋白酶抑制剂，是一种复合蛋白酶抑制剂，具有抗纤维蛋白溶解作用，可抑制接触激活，并可降低对体外循环的炎症反应[2]。抑肽酶抑制胰蛋白酶(牛，Ki = 0.06 pM)，胰凝乳蛋白酶(牛，Ki = 9 nM)，纤溶酶(人，0.23 nM)[1]。抑肽酶也是NOS活性的竞争蛋白抑制剂。它抑制NOS-I和NOS-II，Ki值分别为50μM和78μM[3]。抑肽酶显着抑制纤维蛋白溶解，IC50为0.16±0.05μM[4]。 |
| In Vivo | 高剂量抑肽酶可以减少与原发性心脏手术相关的失血和输血要求，如冠状动脉旁路移植术(CABG)或心脏瓣膜置换手术[5]。抑肽酶以剂量依赖性方式抑制血栓形成。以1.5mg kg-1(推注)和3mg kg-1h-1输注(维持输注)的剂量的抑肽酶导致出血时间减少的趋势。从3mg kg-1推注剂量加6mg kg-1h-1开始，抑肽酶显着减少出血时间，显示减少约84％±2.9％。在最高剂量为5 mg kg-1和10 mg kg-1 h-1时，观察到最强的效果[4]。抑肽酶可能影响肿瘤坏死因子-α(TNF)水平。在抑肽酶处理的野生型小鼠中I / R后可溶性TNFRI水平显着增加，并且在所有TNFRInull小鼠中均未检测到[6]。 |
| Animal Experiment | 大鼠：在研究中使用雄性Wistar大鼠(180-220g)。将抑肽酶溶解在生理盐水中。通过推注注射然后维持输注来施用抑肽酶。给予的剂量是1.5mg kg-1和3mg kg-1h-1，3mg kg-1和6mg kg-1h-1至5mg kg-1和10mg kg-1h-1。通过大鼠的药代动力学研究评估两种药物的血浆浓度[4]。小鼠：使用缺血/再灌注的完整小鼠模型(30分钟-I / 60分钟-R)并且在野生型小鼠(WT，C57BL / 6; n = 10)，WT中测量左心室峰值+ dP / dt。具有抑肽酶(4mL / kg; n = 10)的小鼠，缺乏TNFRI的转基因小鼠(TNFRInull; n = 10)和含有抑肽酶的TNFRInull(n = 10)[6]。 |
| Data Literature Source | [1]. Fritz H， et al. Biochemistry and applications of aprotinin， the kallikrein inhibitor from bovine organs. Arzneimittelforschung. 1983; 33 (4) :479-94. [2]. Levy JH， et al. Efficacy and safety of aprotinin in cardiac surgery. Orthopedics. 2004 Jun; 27 (6 Suppl) :s659-62. [3]. Venturini G， et al. Aprotinin， the first competitive protein inhibitor of NOS activity.Biochem Biophys Res Commun. 1998 Aug 10; 249 (1) :263-5 [4]. Sperzel M， et al. Evaluation of aprotinin and tranexamic acid in different in vitro and in vivo models of fibrinolysis， coagulation and thrombus formation. J Thromb Haemost. 2007 Oct; 5 (10) :2113-8. Epub 2007 Jul 31. [5]. Davis R， et al. Aprotinin. A review of its pharmacology and therapeutic efficacy in reducing blood loss associated withcardiac surgery. Drugs. 1995 Jun; 49 (6) :954-83. [6]. Sabbagh MJ， et al. Aprotinin exacerbates left ventricular dysfunction after ischemia/reperfusion in mice lacking tumor necrosis factor receptor I. J Cardiovasc Pharmacol. 2008 Oct; 52 (4) :355-62. |
| Unit | Bottle |
| Specification | 10mg 50mg 100mg |
Examples of using this product（for reference only）
In Vitro:
Western blotting. （0.3 μM Aprotinin）:
MCF-7 cells were treated with the aforementioned CoCl2 concentrations for 24 h and cells were lysed with ice-cold radioimmunoprecipitation assay buffer (150 mM NaCl, 1.0% NP-40, 0.1% Triton X-100, 0.5% sodium deoxycholate, 0.1% SDS and 50 mM Tris-HCl, pH 8.0) and protease inhibitors (AEBSF at 2 mM, Aprotinin at 0.3 μM, Bestatin at 116 μM, E-64 at 14 μM, Leupeptin at 1 μM and EDTA at 1 mM; Beijing Solarbio Science & Technology Co., Ltd., Beijing, China).
Reference：
Li Q, Ma R, Zhang M. CoCl2 increases the expression of hypoxic markers HIF-1α, VEGF and CXCR4 in breast cancer MCF-7 cells. Oncol Lett. 2018 Jan;15(1):1119-1124. doi: 10.3892/ol.2017.7369. Epub 2017 Nov 8. PMID: 29391899; PMCID: PMC5769392.
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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