Bimakalim   中文名称: 比卡林

1: Alexandre J, Puddu PE, Simard C, Hof T, Sallé L, Guinamard R, Manrique A, Rouet R, Beygui F, Milliez P. Proarrhythmic effects of aldosterone during myocardial ischemia-reperfusion: implication of the sarcolemmal-KATP channels. J Cardiovasc Pharmacol. 2014 Aug;64(2):134-41. doi: 10.1097/FJC.0000000000000097. PMID: 24662493. 2: Aidonidis I, Poyatzi A, Stamatiou G, Lymberi M, Stamatoyannis N, Molyvdas PA. Dose-related shortening of ventricular tachycardia cycle length after administration of the KATP channel opener bimakalim in a 4-day-old chronic infarct anesthetized pig model. J Cardiovasc Pharmacol Ther. 2009 Sep;14(3):222-30. doi: 10.1177/1074248409338929. Epub 2009 Jul 8. PMID: 19587223. 3: Stephan D, Salamon E, Weber H, Russ U, Lemoine H, Quast U. KATP channel openers of the benzopyran type reach their binding site via the cytosol. Br J Pharmacol. 2006 Sep;149(2):199-205. doi: 10.1038/sj.bjp.0706858. Epub 2006 Aug 14. PMID: 16921394; PMCID: PMC2013803. 4: Merkus D, Sorop O, Houweling B, Hoogteijling BA, Duncker DJ. KCa+ channels contribute to exercise-induced coronary vasodilation in swine. Am J Physiol Heart Circ Physiol. 2006 Nov;291(5):H2090-7. doi: 10.1152/ajpheart.00315.2006. Epub 2006 May 12. PMID: 16699076. 5: Gumina RJ, El Schultz J, Moore J, Beier N, Schelling P, Gross GJ. Cardioprotective-mimetics reduce myocardial infarct size in animals resistant to ischemic preconditioning. Cardiovasc Drugs Ther. 2005 Oct;19(5):315-22. doi: 10.1007/s10557-005-3693-8. PMID: 16382293. 6: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2005 Mar;27(2):145-59. PMID: 15834466. 7: Burian M, Piske M, Petkovic D, Mitrovic V. Lack of anti-ischemic efficacy of the potassium channel opener bimakalim in patients with stable angina pectoris. Cardiovasc Drugs Ther. 2004 Jan;18(1):37-46. doi: 10.1023/B:CARD.0000025754.08942.03. PMID: 15115902. 8: Camara AK, Chen Q, Rhodes SS, Riess ML, Stowe DF. Negative inotropic drugs alter indexes of cytosolic [Ca(2+)]-left ventricular pressure relationships after ischemia. Am J Physiol Heart Circ Physiol. 2004 Aug;287(2):H667-80. doi: 10.1152/ajpheart.01142.2003. Epub 2004 Apr 1. PMID: 15059780. 9: Gauthier KM, Jagadeesh SG, Falck JR, Campbell WB. 14,15-epoxyeicosa-5(Z)-enoic-mSI: a 14,15- and 5,6-EET antagonist in bovine coronary arteries. Hypertension. 2003 Oct;42(4):555-61. doi: 10.1161/01.HYP.0000091265.94045.C7. Epub 2003 Sep 2. PMID: 12953017. 10: Fujimoto K, Bosnjak ZJ, Kwok WM. Isoflurane-induced facilitation of the cardiac sarcolemmal K(ATP) channel. Anesthesiology. 2002 Jul;97(1):57-65. doi: 10.1097/00000542-200207000-00009. PMID: 12131104. 11: Gauthier KM, Deeter C, Krishna UM, Reddy YK, Bondlela M, Falck JR, Campbell WB. 14,15-Epoxyeicosa-5(Z)-enoic acid: a selective epoxyeicosatrienoic acid antagonist that inhibits endothelium-dependent hyperpolarization and relaxation in coronary arteries. Circ Res. 2002 May 17;90(9):1028-36. doi: 10.1161/01.res.0000018162.87285.f8. PMID: 12016270. 12: Salamon E, Mannhold R, Weber H, Lemoine H, Frank W. 6-Sulfonylchromenes as highly potent K(ATP)-channel openers. J Med Chem. 2002 Feb 28;45(5):1086-97. doi: 10.1021/jm010999g. PMID: 11855989. 13: Das B, Sarkar C, Karanth KS. Effects of administration of nicorandil or bimakalim prior to and during ischemia or reperfusion on survival rate, ischemia/reperfusion-induced arrhythmias and infarct size in anesthetized rabbits. Naunyn Schmiedebergs Arch Pharmacol. 2001 Nov;364(5):383-96. doi: 10.1007/s002100100457. PMID: 11692221. 14: Pountney DJ, Sun ZQ, Porter LM, Nitabach MN, Nakamura TY, Holmes D, Rosner E, Kaneko M, Manaris T, Holmes TC, Coetzee WA. Is the molecular composition of K(ATP) channels more complex than originally thought? J Mol Cell Cardiol. 2001 Aug;33(8):1541-6. doi: 10.1006/jmcc.2001.1407. PMID: 11448141. 15: Pratt PF, Li P, Hillard CJ, Kurian J, Campbell WB. Endothelium-independent, ouabain-sensitive relaxation of bovine coronary arteries by EETs. Am J Physiol Heart Circ Physiol. 2001 Mar;280(3):H1113-21. doi: 10.1152/ajpheart.2001.280.3.H1113. PMID: 11179054. 16: Eells JT, Henry MM, Gross GJ, Baker JE. Increased mitochondrial K(ATP) channel activity during chronic myocardial hypoxia: is cardioprotection mediated by improved bioenergetics? Circ Res. 2000 Nov 10;87(10):915-21. doi: 10.1161/01.res.87.10.915. PMID: 11073888. 17: Holmes DS, Sun ZQ, Porter LM, Bernstein NE, Chinitz LA, Artman M, Coetzee WA. Amiodarone inhibits cardiac ATP-sensitive potassium channels. J Cardiovasc Electrophysiol. 2000 Oct;11(10):1152-8. doi: 10.1111/j.1540-8167.2000.tb01762.x. PMID: 11059980. 18: Mitrovic V, Oehm E, Thormann J, Pitschner H, Hamm C. Potassium channel openers and blockers in coronary artery disease. Comparison to betablockers and calcium antagonists. Herz. 2000 Mar;25(2):130-42. doi: 10.1007/pl00001951. PMID: 10829253. 19: Buchheit KH, Hofmann A, Manley P, Pfannkuche HJ, Quast U. Atypical effect of minoxidil sulphate on guinea pig airways. Naunyn Schmiedebergs Arch Pharmacol. 2000 Apr;361(4):418-24. doi: 10.1007/s002100000218. PMID: 10763857. 20: Monti F, Iwashiro K, Picard S, Criniti A, La Francesca S, Ruvolo G, Papalia U, Campa PP, Marino B, Puddu PE. Adenosine triphosphate-dependent potassium channel modulation and cardioplegia-induced protection of human atrial muscle in an in vitro model of myocardial stunning. J Thorac Cardiovasc Surg. 2000 Apr;119(4 Pt 1):842-8. doi: 10.1016/S0022-5223(00)70022-5. PMID: 10733778.

C17H14N2O2

278.311

278.106

C, 73.37; H, 5.07; N, 10.07; O, 11.50

117545-11-6

60674

Solid powder

1.29g/cm3

498.4ºC at 760mmHg

255.2ºC

4.56E-10mmHg at 25°C

1.651

2.78

55.02

0

3

1

21

591

0

CC1(C)C=C(N2C=CC=CC2=O)C2C=C(C#N)C=CC=2O1

JTVSKASWNROQQF-UHFFFAOYSA-N

InChI=1S/C17H14N2O2/c1-17(2)10-14(19-8-4-3-5-16(19)20)13-9-12(11-18)6-7-15(13)21-17/h3-10H,1-2H3

2,2-dimethyl-4-(2-oxopyridin-1(2H)-yl)-2H-chromene-6-carbonitrile

Bimakalim; EMD 52692; EMD-52692; EMD52692; SR 44866; SR-44866; SR44866;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。