7-Piperazin-1-yl-thieno[2,3-c] Pyridine (hydrochloride)
(Synonyms: 7-(1-哌嗪基)噻吩并[2,3-C]吡啶盐酸盐) 目录号 : GC42618Synthetic intermediate
Cas No.:850734-85-9
Sample solution is provided at 25 µL, 10mM.
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- Purity: >98.00%
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tert-butyl p-Toluate is a synthetic intermediate useful for pharmaceutical synthesis.
Cas No. | 850734-85-9 | SDF | |
别名 | 7-(1-哌嗪基)噻吩并[2,3-C]吡啶盐酸盐 | ||
Canonical SMILES | C1(C=CS2)=C2C(N3CCNCC3)=NC=C1.Cl | ||
分子式 | C11H13N3S•HCl | 分子量 | 255.8 |
溶解度 | DMF: 1 mg/ml,DMSO: 20 mg/ml,Ethanol: 0.15 mg/ml,PBS (pH 7.2): 10 mg/ml | 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 | 3.9093 mL | 19.5465 mL | 39.093 mL |
5 mM | 0.7819 mL | 3.9093 mL | 7.8186 mL |
10 mM | 0.3909 mL | 1.9547 mL | 3.9093 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 | ||||||||||
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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。
Bioassay of 2-(Chloromethyl)Pyridine hydrochloride for Possible Carcinogenicity (CAS No. 6959-47-3)
Natl Toxicol Program Tech Rep Ser 1979;178:1-97.PMID:12778175doi
2-(Chloromethyl)pyridine hydrochloride, an aromatic heterocycle used in a variety of syntheses, was selected for bioassay by the National Cancer Institute because of the structural similarity of this compound to 2-(a,b-dichloroethyl)-pyridine hydrochloride, a carcinogen in rats, mice, Syrian hamsters, and Mongolian gerbils. A bioassay for the possible carcinogenicity of 2-(chloromethyl)pyridine hydrochloride was conducted using Fischer 344 rats and B6C3F1 mice. 2-(Chloromethyl)pyridine hydrochloride was administered by gavage, at either of two dosages, to groups of 50 male and 50 female animals of each species, with the exception of 49 male rats in the high dose group. Twenty animals of each sex and species were placed on test as vehicle controls. The high and low dosages of 2-(chloromethyl)pyridine hydrochloride administered were, respectively, 150 and 75 mg/kg for rats and 250 and 125 mg/kg for mice. The compound was administered for 99 weeks to rats and mice. The period of compound administration was followed by an observation period of 6 weeks for rats and 5 weeks for mice. There were no significant positive associations between the dosages of 2-(chloromethyl)pyridine hydrochloride administered and mortality in rats or mice of either sex. Adequate numbers of animals in all groups survived sufficiently long to be at risk from late-developing tumors. Slight dose-related mean body weight depression was observed in mice of both sexes, indicating that the dosages of 2-(chloromethyl)pyridine hydrochloride administered tothese animals in this bioassay may have approximated the maximum tolerated concentrations. Since no distinct mean body weight depression relative to vehicle controls, no significant accelerated mortality, and no other signs of toxicity were associated with administration of 2-(chloromethyl)pyridine hydrochloride to rats, it is possible that these animals may have been able to tolerate a higher dosage. None of the statistical tests for any site in female rats or in mice of either sex indicated a significant positive association between compound administration and tumor incidence. There was a significant positive trend between the dosages administered and the incidences of subcutaneous fibromas in male rats. The Fisher exact comparisons, however, were not significant. Under the conditions of this bioassay, administration of 2-(chloromethyl)pyridine hydrochloride was not carcinogenic to Fischer 344 rats or B6C3F1 mice. Levels of Evidence of Carcinogenicity: Male Rats: Negative Female Rats: Negative Male Mice: Negative Female Mice: Negative Synonyms: 2-(Cl-methyl)pyridineHCl; 2-pyridylmethyl chloride hydrochloride; 2-picolylchloride hydrochloride
Efficient regioselective five-component synthesis of novel thiazolo[3,2-a]pyridine carbohydrazides and oxazolo[3,2-a]pyridine carbohydrazides
Mol Divers 2023 Apr;27(2):667-678.PMID:35587848DOI:10.1007/s11030-022-10446-0.
Two new categories of fused pyridines include 2H-thiazolo[3,2-a]pyridine-6-carbohydrazides and 2H-oxazolo[3,2-a]pyridine-6-carbohydrazides have been successfully synthesized via five-component cascade reactions using 9-fluorenone, cyanoacetohydrazide, 1,1-bis(methylthio)-2-nitroethene, aromatic aldehydes and cysteamine hydrochloride or ethanol amine as starting materials. This new approach involves a subsequence of key steps: N,S-acetal or N,O-acetal formation, Knoevenagel condensation, Michael addition, tautomerization and N-cyclization. It also has some advantages, such as convenience of operation, tolerance of a wide diversity of functional groups, use of green solvent and ease of purification by washing the crude products with ethanol.
Antiproliferative and endothelium-dependent vasodilator properties of 1,3-dihydro-3-p-chlorophenyl-7-hydroxy-6-methyl-furo-(3,4c) pyridine hydrochloride (cicletanine)
J Pharmacol Exp Ther 1993 Apr;265(1):30-5.PMID:8474013doi
The vasodilator and antiproliferative actions of 1,3-dihydro-3-p-chlorophenyl-7-hydroxy-6-methyl-furo-(3,4c) pyridine hydrochloride (cicletanine) were studied on mesenteric resistance arteries and cultured mesenteric artery myocytes of spontaneously hypertensive (SHR) and normotensive Wistar Kyoto (WKY) rats. Cicletanine (20-200 microM) induced relaxation of endothelium-intact mesenteric resistance arteries of SHR and WKY precontracted with norepinephrine. No difference in sensitivity was observed (SHR IC50 = 77 +/- 12 microM vs. 83.3 +/- 7.4 microM for WKY, N.S.). Endothelial denudation of WKY vessels significantly attenuated the relaxing action of cicletanine (IC50 + endo = 83 +/- 7.4 microM vs. IC50 - endo = 135 +/- 9.7 microM; P < .001) and had a similar, but nonsignificant effect on SHR (IC50 + endo = 77 +/- 12 microM vs. IC50 - endo = 117 +/- 14.5 microM; P = .065). Preincubation of endothelium-intact vessels with nitro-L-arginine methyl ester significantly attenuated cicletanine-induced relaxation in WKY, but not SHR vessels; 0.1 mM Ba++ had a similar effect. Preincubation with 3 microM indomethacin was without effect on relaxation of vessels of either strain. Cicletanine (100-1000 microM) inhibited proliferation of cultured superior mesenteric artery muscle cells growing in the presence of either 10% (SHR IC50 = 440 +/- 24 microM vs. 517 +/- 12 microM for WKY; P < .05) or 2% fetal bovine serum. This antiproliferative action was fully reversible, partially inhibited by indomethacin in SHR myocytes and was associated with a decrease in [3H]thymidine uptake in both strains.(ABSTRACT TRUNCATED AT 250 WORDS)