TRAM-34,K Ca 3.1通道阻滞剂

强大的选择性K Ca 3.1通道阻滞剂

规格或纯度: ≥98%

CAS编号: 289905-88-0
分子式: C₂₂H₁₇ClN₂
分子量: 344.84
MDL号: MFCD09842562
PubChem编号: 656734

有货

库存信息

关闭

库存信息

关闭

库存信息

关闭

库存信息

关闭

货号 (SKU)	包装规格	是否现货
T129575-5mg	5mg	现货
T129575-25mg	25mg	现货
T129575-50mg	50mg	期货
T129575-100mg	100mg	期货

查看相关系列

KCa3.1 Channel blocker

Skip to the end of the images gallery

Skip to the beginning of the images gallery

基本描述

规格或纯度	≥98%
英文名称	TRAM-34
别名	1-[(2-氯苯基)二苯甲基]-1H-吡唑
英文别名	1-[(2-Chlorophenyl)diphenylmethyl]-1H-pyrazole
生化机理	高效的选择性K Ca 3.1通道阻滞剂（IC 50 = 18 nM）。动脉粥样硬化和免疫抑制剂。在体外和体内具有活性。
储存温度	-20°C储存
运输条件	超低温冰袋运输
备注	如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍	TRAM-34 has been shown to be an inhibitor of cloned and native IK1 channels in human T lymphocytes. These K+ channels have been implicated in over-proliferation of cells. Inhibition of IK1 channels has been demonstrated to modulate cell proliferation depending on the concentration of TRAM-34. Mechanistic studies have shown that TRAM-34 may cause a halt in cell growth at the G0/G1 phase.TRAM-34 is a selective and potent inhibitor of the intermediate-conductance Ca2+-activated K+ channel (IKCa1, KCa3.1) with Kd of 20 nM, 200- to 1500-fold selective over other ion channels, and does not block cytochrome P450. TRAM-34 has been shown to be an inhibitor of cloned and native IK1 channels in human T lymphocytes. These K+ channels have been implicated in over-proliferation of cells. Inhibition of IK1 channels has been demonstrated to modulate cell proliferation depending on the concentration of TRAM-34. Mechanistic studies have shown that TRAM-34 may cause a halt in cell growth at the G0/G1 phase. TRAM-34是一种有效的，选择性的中电导Ca2+-activated K+ channel (IKCa1， KCa3.1)（钙激活的K+通道）抑制剂，Kd为20 nM，比作用于其他离子通道选择性高200到1500倍，且不抑制细胞色素P450。

名称和标识符

IUPAC Name	1-[(2-chlorophenyl)-diphenylmethyl]pyrazole
INCHI	InChI=1S/C22H17ClN2/c23-21-15-8-7-14-20(21)22(25-17-9-16-24-25,18-10-3-1-4-11-18)19-12-5-2-6-13-19/h1-17H
InChi Key	KBFUQFVFYYBHBT-UHFFFAOYSA-N
Canonical SMILES	C1=CC=C(C=C1)C(C2=CC=CC=C2)(C3=CC=CC=C3Cl)N4C=CC=N4
分子式	C₂₂H₁₇ClN₂
PubChem CID	656734
分子量	344.84

数据库链接

PubChem CID	656734
ChEMBL Ligand	CHEMBL498270
BindingDB Ligand	50279107
CAS Registry No.	289905-88-0

化学和物理性质

溶解性	Soluble in DMSO (10 mg/ml at 40°C), ethanol (6 mg/ml at 40°C), and DMF (>25 mg/ml), dichloromethane, ethyl acetate, and methanol. Insoluble in water.

安全信息

象形图	Harmful
信号词	Warning
危险声明	H413: May cause long lasting harmful effects to aquatic life H302: Harmful if swallowed
预防措施声明	P273,P501,P264,P270,P330,P301+P317
WGK Germany	3
个人防护装备	dust mask type N95 (US), Eyeshields, Gloves

靶标

Target ID

384

名称

K_Ca3.1

缩写名

SHP2

家族

Calcium- and sodium-activated potassium channels (K_Ca, K_Na)

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	6	427	19q13.31	KCNN4	potassium calcium-activated channel subfamily N member 4
Rat	6	425	1q21	Kcnn4	potassium calcium-activated channel subfamily N member 4
Mouse	6	425	7 A3	Kcnn4	potassium intermediate/small conductance calcium-activated channel, subfamily N, member 4

OMIM

602754 (Hs)

Entrez Gene

65206 (Rn) , 16534 (Mm) , 3783 (Hs)

UniProtKB

Q9QYW1 (Rn) , O15554 (Hs) , O89109 (Mm)

RefSeq Protein

NP_002241 (Hs) , NP_075410 (Rn) , NP_032459 (Mm)

RefSeq Nucleotide

NM_002250 (Hs) , NM_023021 (Rn) , NM_008433 (Mm)

Ensembl Gene

ENSG00000104783 (Hs) , ENSMUSG00000054342 (Mm) , ENSRNOG00000019440 (Rn)

Protein GI

12711688 (Rn) , 4504859 (Hs) , 254553466 (Mm)

DrugBank Target

O15554 (Hs)

ChEMBL Target

CHEMBL4305 (Hs)

关联配体

Ligand ID	2336
名称	TRAM-34
类别	Synthetic organic
学名	1-[(2-chlorophenyl)-di(phenyl)methyl]pyrazole
生物活性评价	The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价	TRAM-34 is a K_Ca3.1 channel blocker.

参考文献

1. Hua X, Deuse T, Chen YJ, Wulff H, Stubbendorff M, K?hler R, Miura H, L?nger F, Reichenspurner H, Robbins RC et al.. (2013) The potassium channel KCa3.1 as new therapeutic target for the prevention of obliterative airway disease.. Transplantation, 95 (2): (285-92). [PMID:23325003]
2. Yu ZH, Xu JR, Wang YX, Xu GN, Xu ZP, Yang K, Wu DZ, Cui YY, Chen HZ. (2013) Targeted inhibition of KCa3.1 channel attenuates airway inflammation and remodeling in allergic asthma.. Am J Respir Cell Mol Biol, 48 (6): (685-93). [PMID:23492185]
3. Koshy S, Wu D, Hu X, Tajhya RB, Huq R, Khan FS, Pennington MW, Wulff H, Yotnda P, Beeton C. (2013) Blocking KCa3.1 channels increases tumor cell killing by a subpopulation of human natural killer lymphocytes.. PLoS ONE, 8 (10): (e76740). [PMID:24146918]
4. Chimote AA, Hajdu P, Kucher V, Boiko N, Kuras Z, Szilagyi O, Yun YH, Conforti L. (2013) Selective inhibition of KCa3.1 channels mediates adenosine regulation of the motility of human T cells.. J Immunol, 191 (12): (6273-80). [PMID:24227782]
5. Chen YJ, Lam J, Gregory CR, Schrepfer S, Wulff H. (2013) The Ca2?-activated K? channel KCa3.1 as a potential new target for the prevention of allograft vasculopathy.. PLoS ONE, 8 (11): (e81006). [PMID:24312257]
6. Roach KM, Duffy SM, Coward W, Feghali-Bostwick C, Wulff H, Bradding P. (2013) The K+ channel KCa3.1 as a novel target for idiopathic pulmonary fibrosis.. PLoS ONE, 8 (12): (e85244). [PMID:24392001]
7. Crottès D, Félix R, Meley D, Chadet S, Herr F, Audiger C, Soriani O, Vandier C, Roger S, Angoulvant D et al.. (2016) Immature human dendritic cells enhance their migration through KCa3.1 channel activation.. Cell Calcium, 59 (4): (198-207). [PMID:27020659]
8. Glaser N, Little C, Lo W, Cohen M, Tancredi D, Wulff H, O'Donnell M. (2017) Treatment with the KCa3.1 inhibitor TRAM-34 during diabetic ketoacidosis reduces inflammatory changes in the brain.. Pediatr Diabetes, 18 (5): (356-366). [PMID:27174668]
9. Ohya S, Fukuyo Y, Kito H, Shibaoka R, Matsui M, Niguma H, Maeda Y, Yamamura H, Fujii M, Kimura K et al.. (2014) Upregulation of KCa3.1 K(+) channel in mesenteric lymph node CD4(+) T lymphocytes from a mouse model of dextran sodium sulfate-induced inflammatory bowel disease.. Am J Physiol Gastrointest Liver Physiol, 306 (10): (G873-85). [PMID:24674776]
10. Chen YJ, Nguyen HM, Maezawa I, Gr?ssinger EM, Garing AL, K?hler R, Jin LW, Wulff H. (2016) The potassium channel KCa3.1 constitutes a pharmacological target for neuroinflammation associated with ischemia/reperfusion stroke.. J Cereb Blood Flow Metab, 36 (12): (2146-2161). [PMID:26661208]
11. Zhang S, Wang X, Ju C, Zhu L, Du Y, Gao C. (2016) Blockage of K(Ca)3.1 and Kv1.3 channels of the B lymphocyte decreases the inflammatory monocyte chemotaxis.. Int Immunopharmacol, 31 (13): (266-71). [PMID:26795234]
12. Lin H, Zheng C, Li J, Yang C, Hu L. (2014) Ca2+ -activated K+ channel-3.1 blocker TRAM-34 alleviates murine allergic rhinitis.. Int Immunopharmacol, 23 (2): (642-8). [PMID:25466273]
13. Friebel K, Sch?nherr R, Kinne RW, Kunisch E. (2015) Functional role of the KCa3.1 potassium channel in synovial fibroblasts from rheumatoid arthritis patients.. J Cell Physiol, 230 (7): (1677-88). [PMID:25545021]
14. Shao Z, Gaurav R, Agrawal DK. (2015) Intermediate-conductance calcium-activated potassium channel KCa3.1 and chloride channel modulate chemokine ligand (CCL19/CCL21)-induced migration of dendritic cells.. Transl Res, 166 (1): (89-102). [PMID:25583444]

产品问答

登录提交问题

查看全部

您提交该产品问题后,我们会在1-2个工作日内给您答复,您可以登录"我的账号",然后点击"我的产品问答"查看答案

91高清自产国产拍,无码免费A级毛片大全,日本欧美国产中文字幕,99re热视频这里只有精品视频首页

TRAM-34,K Ca 3.1通道阻滞剂

库存信息

库存信息

库存信息

库存信息

基本描述

名称和标识符

数据库链接

化学和物理性质

安全信息

靶标

关联配体

参考文献

相关文档

质检报告COA

产品问答

产品问答

91高清自产国产拍,无码免费A级毛片大全,日本欧美国产中文字幕,99re热视频这里只有精品视频首页

91高清自产国产拍,无码免费A级毛片大全,日本 欧美 国产中文字幕,99re热视频这里只有精品视频首页

TRAM-34,K Ca 3.1通道阻滞剂

库存信息

库存信息

库存信息

库存信息

基本描述

名称和标识符

数据库链接

化学和物理性质

安全信息

靶标

关联配体

参考文献

相关文档

质检报告COA

产品问答

产品问答

91高清自产国产拍,无码免费A级毛片大全,日本 欧美 国产中文字幕,99re热视频这里只有精品视频首页

91高清自产国产拍,无码免费A级毛片大全,日本欧美国产中文字幕,99re热视频这里只有精品视频首页

91高清自产国产拍,无码免费A级毛片大全,日本欧美国产中文字幕,99re热视频这里只有精品视频首页