N-PTyrosine PA ammonium
N-PTyrosine PA (N-Palmitoyl-tyrosine phosphoric acid) ammonium is a lysophosphatidic acid (LPA) receptor modulator, which exhibits weak inhibitory activity against LPA1 and partial agonist properties towards LPA5. N-PTyrosine PA ammonium inhibits the activation of LPA receptors and downstream responses by competing with agonists for binding sites. N-PTyrosine PA ammonium can induce morphological changes and aggregation, and also inhibit LPA-induced morphological changes through receptor desensitization caused by pre-incubation. N-PTyrosine PA ammonium can be used in the research of related diseases such as atherosclerosis and acute ischemic syndromes (e.g., unstable angina, myocardial infarction, stroke).
For research use only. We do not sell to patients.
- CAS No.: 799268-45-4
- Formula: C25H45N2O7P
- Molecular Weight:516.61
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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LPA5 Receptor |
N-PTyrosine PA ammonium (1 μM; 10 min) inhibits the lysophosphatidic acid receptor-mediated oscillatory inward Cl- current by 69.8% in non-injected Xenopus oocytes, and this inhibition is fully reversible after washing[1].
N-PTyrosine PA ammonium induces morphological changes in human platelets with an EC50 of 0.2-0.3 μM; after 30 min of pre-incubation, N-PTyrosine PA ammonium inhibits LPA-induced morphological changes in human platelets with an IC50 of 0.2-0.3 μM[2].
N-PTyrosine PA ammonium acts as a partial micromolar agonist of the LPA5 receptor in transiently transfected RH7777 cells, exerts weak inhibitory activity against the LPA1 receptor in stably transfected RH7777 cells with a Ki of 533 nM, and shows no activity towards the LPA2, LPA3 or LPA4 receptor[2].
N-PTyrosine PA ammonium (10-30 μM; 5 min) does not induce Na+-dependent Ca2+ efflux in cultured bovine adrenal chromaffin cells at a concentration of 10 μM, nor does it inhibit 18:1-LPA (HY-157725)-stimulated Ca2+ efflux at concentrations of 10 μM or 30 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Cultured bovine adrenal chromaffin cells
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Concentration:10-30 μM
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Incubation Time:5 min
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Result:Couldn't induce Na+-dependent Ca2+ efflux in cultured bovine adrenal chromaffin cells at a concentration of 10 μM。
Chemical Information
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CAS No. 799268-45-4
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Molecular Weight 516.61
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Formula C25H45N2O7P
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SMILES
CCCCCCCCCCCCCCCC(N[C@H](C(O)=O)CC1=CC=C(C=C1)OP(O)(O)=O)=O.N
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Synonyms
N-Palmitoyl-tyrosine phosphoric acid ammonium
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Stankiewicz M, et al. Effects of a centipede venom fraction on insect nervous system, a native Xenopus oocyte receptor and on an expressed Drosophila muscarinic receptor. Toxicon. 1999;37(10):1431-1445. [Content Brief]
[2]. Khandoga AL, et al. Lysophosphatidic acid-induced platelet shape change revealed through LPA(1-5) receptor-selective probes and albumin. Platelets. 2008;19(6):415-427. [Content Brief]
[3]. Tokumura A, et al. Positive and negative controls by protein kinases of sodium-dependent Ca2+ efflux from cultured bovine adrenal chromaffin cells stimulated by lysophosphatidic acid. Biochim Biophys Acta. 1998;1389(1):67-75. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
N-PTyrosine PA ammonium Related Classifications
HY-W040176 Related Classifications
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