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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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T129575-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $24.90 | |
T129575-25mg | 25mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $102.90 | |
T129575-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $195.90 | |
T129575-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $352.90 |
Potent, selective K Ca 3.1 channel blocker
Synonyms | TRAM-34|289905-88-0|1-((2-chlorophenyl)diphenylmethyl)-1H-pyrazole|1-[(2-Chlorophenyl)diphenylmethyl]-1H-pyrazole|Tram 34|TRAM34|Triarylmethane-34|C22H17ClN2|1-[(2-chlorophenyl)-diphenylmethyl]pyrazole|CHEMBL498270|CHEBI:34990|1H-Pyrazole, 1-[(2-chlorophe |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Potent, selective K Ca 3.1 channel blocker (IC 50 = 18 nM). Atherosclerosis and immunosuppressive agent. Active in vitro and in vivo . |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | CHANNEL BLOCKER |
Mechanism of action | Channel blocker of K Ca3.1 |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | 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. |
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IUPAC Name | 1-[(2-chlorophenyl)-diphenylmethyl]pyrazole |
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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 |
Isomeric SMILES | C1=CC=C(C=C1)C(C2=CC=CC=C2)(C3=CC=CC=C3Cl)N4C=CC=N4 |
WGK Germany | 3 |
PubChem CID | 656734 |
Molecular Weight | 344.84 |
PubChem CID | 656734 |
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ChEMBL Ligand | CHEMBL498270 |
BindingDB Ligand | 50279107 |
CAS Registry No. | 289905-88-0 |
Enter Lot Number to search for COA:
To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section
Lot Number | Certificate Type | Date | Item |
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D1524067 | Certificate of Analysis | Nov 15, 2022 | T129575 |
Solubility | 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. |
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Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H413:May cause long lasting harmful effects to aquatic life H302:Harmful if swallowed |
Precautionary Statements | P273:Avoid release to the environment. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P270:Do not eat, drink or smoke when using this product. P330:Rinse mouth. P301+P317:IF SWALLOWED: Get medical help. |
WGK Germany | 3 |
1. Hua X, Deuse T, Chen YJ, Wulff H, Stubbendorff M, Köhler R, Miura H, Länger 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, Grössinger EM, Garing AL, Köhler 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 (3): (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, Schönherr 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] |