U-73343
U-73343 is a negative control (or inactive analogue) of U73122, which is a putative phospholipase C inhibitor. U73343 was found to inhibit TxA2 formation; it therefore partially inhibited the rise in [Ca2+]i evoked by low concentrations of thrombin, by thapsigargin or by collagen. U73343 had a greater effect than aspirin on the action of collagen, indicating an action on the TxA2-independent component of the signal, via PLC gamma-U73343 lowered TxA2 production by inhibiting the activation of cPLA2, probably at a tyrosine phosphorylation step. U73343 seems to inhibit only the tyrosine kinases involved in the activation of PLC gamma and the generation of TxA2.
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Chemical Information
| Name | U-73343 |
|---|---|
| Iupac Chemical Name | 1-(6-(((8R,9S,13S,14S,17S)-3-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-17-yl)amino)hexyl)pyrrolidine-2,5-dione |
| Synonyms | U73343, U-73343, U 73343 |
| Molecular Formula | C29H42N2O3 |
| Molecular Weight | 466.66 |
| Smile | COC=1C=CC=2[C@H]3CC[C@@]4([C@H](CC[C@H]4[C@@H]3CCC2C1)NCCCCCCN1C(CCC1=O)=O)C |
| InChiKey | CJHWFIUASFBCKN-ZRJUGLEFSA-N |
| InChi | InChI=1S/C29H42N2O3/c1-29-16-15-23-22-10-8-21(34-2)19-20(22)7-9-24(23)25(29)11-12-26(29)30-17-5-3-4-6-18-31-27(32)13-14-28(31)33/h8,10,19,23-26,30H,3-7,9,11-18H2,1-2H3/t23-,24-,25+,26+,29+/m1/s1 |
| CAS Number | 142878-12-4 |
| Related CAS | 142878-12-4 |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Off-white solid to white solid |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO, not in water |
| Handling | |
| Shipping Condition | Shipped under ambient temperature |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Takenouchi T, Ogihara K, Sato M, Kitani H. Inhibitory effects of U73122 and U73343 on Ca2+ influx and pore formation induced by the activation of P2X7 nucleotide receptors in mouse microglial cell line. Biochim Biophys Acta. 2005 Nov 15;1726(2):177-86. Epub 2005 Aug 15. PubMed PMID: 16122875.
2: Bosch RR, Patel AM, Van Emst-de Vries SE, Smeets RL, De Pont JJ, Willems PH. U73122 and U73343 inhibit receptor-mediated phospholipase D activation downstream of phospholipase C in CHO cells. Eur J Pharmacol. 1998 Apr 10;346(2-3):345-51. PubMed PMID: 9652379.
3: Muto Y, Nagao T, Urushidani T. The putative phospholipase C inhibitor U73122 and its negative control, U73343, elicit unexpected effects on the rabbit parietal cell. J Pharmacol Exp Ther. 1997 Sep;282(3):1379-88. PubMed PMID: 9316850.
4: Heemskerk JW, Feijge MA, Sage SO, Farndale RW. Human platelet activation is inhibited upstream of the activation of phospholipase A2 by U73343. Biochem Pharmacol. 1997 May 9;53(9):1257-62. PubMed PMID: 9214686.
5: Heemskerk JW, Farndale RW, Sage SO. Effects of U73122 and U73343 on human platelet calcium signalling and protein tyrosine phosphorylation. Biochim Biophys Acta. 1997 Jan 10;1355(1):81-8. PubMed PMID: 9030204.
Chemical Structure
