Danegaptide
(Synonyms: (2S,4R)-1-(2-氨基乙酰基)-4-苯甲酰胺吡咯烷-2-甲酸,GAP-134; ZP 1609) 目录号 : GC35806Danegaptide (GAP-134) 是修饰的二肽,是第二代口服生物相容性的间隙连接调节剂。
Cas No.:943134-39-2
Sample solution is provided at 25 µL, 10mM.
Danegaptide (GAP-134), a small modified dipeptide, has been identified as a potent and selective second generation gap junction modifier with oral bioavailability. Gap junction.
Gap junction uncoupling can alter conduction pathways and promote cardiac re-entry mechanisms that potentiate many supraventricular arrhythmias, such as atrial fibrillation (AF) and atrial flutter (AFL). Gap junction modifier Danegaptide (GAP-134), showed consistent efficacy on measures of conduction and AF/AFL inducibility in the canine sterile pericarditis model. Danegaptide (GAP-134) is a pharmalogical agent with a favorable clinical safety profile and potential antiarrhythmic efficacy, as already confirmed in phase I clinical trials.
[1]. De Vuyst E, Boengler K, Antoons G, et al. Pharmacological modulation of connexin-formed channels in cardiac pathophysiology. Br J Pharmacol. 2011 Jun;163(3):469-83. [2]. Laurent G, Leong-Poi H, Mangat I, et al. Effects of chronic gap junction conduction-enhancing antiarrhythmic peptide GAP-134 administration on experimental atrial fibrillation in dogs. Circ Arrhythm Electrophysiol. 2009 Apr;2(2):171-8. [3]. Hennan JK, Swillo RE, Morgan GA, et al. GAP-134 ([2S,4R]-1-[2-aminoacetyl]4-benzamidopyrrolidine-2-carboxylic acid) prevents spontaneous ventricular arrhythmias and reduces infarct size during myocardial ischemia/reperfusion injury in open-chest dogs. J Cardiovasc Pharmacol Ther. 2009 Sep;14(3):207-14. [4]. Rossman EI, Liu K, Morgan GA, et al. The gap junction modifier, GAP-134 [(2S,4R)-1-(2-aminoacetyl)-4-benzamido-pyrrolidine-2-carboxylic acid], improves conduction and reduces atrial fibrillation/flutter in the canine sterile pericarditis model. J Pharmacol Exp Ther. 2009 Jun;329(3):1127-33. [5]. Eugene L. Piatnitski Cheklera, John A. Buterab, Li Dib, Discovery of a class of potent gap-junction modifiers as novel antiarrhythmic agents. Bioorganic & Medicinal Chemistry Letters. 2009,19(16): 4551-4554
Cas No. | 943134-39-2 | SDF | |
别名 | (2S,4R)-1-(2-氨基乙酰基)-4-苯甲酰胺吡咯烷-2-甲酸,GAP-134; ZP 1609 | ||
Canonical SMILES | O=C(N[C@H]1CN(C(CN)=O)[C@H](C(O)=O)C1)C2=CC=CC=C2 | ||
分子式 | C14H17N3O4 | 分子量 | 291.3 |
溶解度 | Soluble in DMSO | 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.4329 mL | 17.1644 mL | 34.3289 mL |
5 mM | 0.6866 mL | 3.4329 mL | 6.8658 mL |
10 mM | 0.3433 mL | 1.7164 mL | 3.4329 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。
Quality Control & SDS
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- Purity: >98.00%
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Related Biological Data
ZP1609 promotes GJs-CX43 expression and reconstitutes GJ-mediated astrocyte network, and inhibits the infammatory response of primary astrocytes after receiving a long-term isofurane anesthesia. ZP1609 alleviated long-term isofurane exposure-induced increased levels of IL-1β (k) and IL-6 (l) in primary astrocytes.
Mice were treated with Danegaptide (ZP1609) (dosage: 300µg/kg every time, three times/day) (GLPBIO, USA) by intraperitoneal injection for 3 consecutive days after the mice model was established.
Journal of Neuroinflammation 19.1 (2022): 1-22. PMID: 35255943 IF: 8.3222 -
Related Biological Data
Enhanced gap junctions Connexin43 coupling can alleviate cognitive dysfunction induced by long-term isoflurane anesthesia. Cognitive functions are impaired in mice after long-term isoflurane anesthesia and treatment with Danegaptide significantly improved the contextual fear memory (A).
After 30min of treatment with Danegaptide (ZP1609) (1μg/ml, GLPBIO, USA), the total Cx43 notably decreased in isoflurane-treated primary astrocytes and was not reversed by Danegaptide.
CNS Neuroscience & Therapeutics (2022). PMID: 36153812 IF: 7.0348