P-1075
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 529713

CAS#: 60559-98-0

Description: P-1075, also known as PNU-83757 and U-83757, is a K-ATP channel agonist potentially for the treatment of erectile dysfunction, alopecia and arrhythmia.


Price and Availability

Size
Price

10mg
USD 330
Size
Price

50mg
USD 990
Size
Price

P-1075, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 529713
Name: P-1075
CAS#: 60559-98-0
Chemical Formula: C12H17N5
Exact Mass: 231.1484
Molecular Weight: 231.3
Elemental Analysis: C, 62.31; H, 7.41; N, 30.28


Synonym: P-1075; PNU-83757; U-83757; P1075; PNU83757; U83757; P 1075; PNU 83757; U 83757

IUPAC/Chemical Name: N-cyano-N'-(1,1-dimethylpropyl)-N''-(3-pyridinyl)guanidine

InChi Key: HKZNADVVGXKQDL-UHFFFAOYSA-N

InChi Code: InChI=1S/C12H17N5/c1-4-12(2,3)17-11(15-9-13)16-10-6-5-7-14-8-10/h5-8H,4H2,1-3H3,(H2,15,16,17)

SMILES Code: CCC(N/C(NC#N)=N/C1=CC=CN=C1)(C)C


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
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

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Ng B, Kang Y, Xie H, Sun H, Gaisano HY. Syntaxin-1A inhibition of P-1075, cromakalim, and diazoxide actions on mouse cardiac ATP-sensitive potassium channel. Cardiovasc Res. 2008 Dec 1;80(3):365-74. doi: 10.1093/cvr/cvn210. PubMed PMID: 18703534.

2: Sato T, Nakaya H. P-1075 exerts diverse modulatory effects on mitochondrial ATP-sensitive K+ channels in rabbit ventricular myocytes. J Cardiovasc Pharmacol. 2006 Feb;47(2):165-8. PubMed PMID: 16495751.

3: Jilkina O, Kuzio B, Grover GJ, Folmes CD, Kong HJ, Kupriyanov VV. Sarcolemmal and mitochondrial effects of a KATP opener, P-1075, in "polarized" and "depolarized" Langendorff-perfused rat hearts. Biochim Biophys Acta. 2003 Dec 3;1618(1):39-50. PubMed PMID: 14643932.

4: Jilkina O, Kuzio B, Grover GJ, Kupriyanov VV. Cardioselective sulfonylthiourea HMR 1098 blocks mitochondrial uncoupling induced by a KATP channel opener, P-1075, in beating rat hearts. Biochim Biophys Acta. 2003 Jul 14;1638(2):121-8. PubMed PMID: 12853117.

5: Jilkina O, Kuzio B, Grover GJ, Kupriyanov VV. Effects of K(ATP) channel openers, P-1075, pinacidil, and diazoxide, on energetics and contractile function in isolated rat hearts. J Mol Cell Cardiol. 2002 Apr;34(4):427-40. PubMed PMID: 11991732.

6: Jilkina O, Kuzio B, Kupriyanov VV. Potassium fluxes, energy metabolism, and oxygenation in intact diabetic rat hearts under normal and stress conditions. Can J Physiol Pharmacol. 2008 Oct;86(10):710-25. doi: 10.1139/y08-076. PubMed PMID: 18841176.

7: Jansen-Olesen I, Mortensen CH, El-Bariaki N, Ploug KB. Characterization of K(ATP)-channels in rat basilar and middle cerebral arteries: studies of vasomotor responses and mRNA expression. Eur J Pharmacol. 2005 Oct 31;523(1-3):109-18. PubMed PMID: 16226739.

8: Ploug KB, Boni LJ, Baun M, Hay-Schmidt A, Olesen J, Jansen-Olesen I. K(ATP) channel expression and pharmacological in vivo and in vitro studies of the K(ATP) channel blocker PNU-37883A in rat middle meningeal arteries. Br J Pharmacol. 2008 May;154(1):72-81. doi: 10.1038/bjp.2008.86. PubMed PMID: 18332850; PubMed Central PMCID: PMC2438990.

9: Sargent CA, Sleph PG, Dzwonczyk S, Normandin D, Antonaccio MJ, Grover GJ. Cardioprotective effects of the cyanoguanidine potassium channel opener P-1075. J Cardiovasc Pharmacol. 1993 Oct;22(4):564-70. PubMed PMID: 7505358.

10: Sato T, Sasaki N, Seharaseyon J, O'Rourke B, Marbán E. Selective pharmacological agents implicate mitochondrial but not sarcolemmal K(ATP) channels in ischemic cardioprotection. Circulation. 2000 May 23;101(20):2418-23. PubMed PMID: 10821820.

11: Gross ER, Hsu AK, Gross GJ. GSK3beta inhibition and K(ATP) channel opening mediate acute opioid-induced cardioprotection at reperfusion. Basic Res Cardiol. 2007 Jul;102(4):341-9. PubMed PMID: 17450314.

12: Liu Y, Ren G, O'Rourke B, Marbán E, Seharaseyon J. Pharmacological comparison of native mitochondrial K(ATP) channels with molecularly defined surface K(ATP) channels. Mol Pharmacol. 2001 Feb;59(2):225-30. PubMed PMID: 11160857.

13: Baczkó I, Jones L, McGuigan CF, Manning Fox JE, Gandhi M, Giles WR, Clanachan AS, Light PE. Plasma membrane KATP channel-mediated cardioprotection involves posthypoxic reductions in calcium overload and contractile dysfunction: mechanistic insights into cardioplegia. FASEB J. 2005 Jun;19(8):980-2. PubMed PMID: 15774423.

14: Cao C, Lee-Kwon W, Silldorff EP, Pallone TL. KATP channel conductance of descending vasa recta pericytes. Am J Physiol Renal Physiol. 2005 Dec;289(6):F1235-45. PubMed PMID: 16048905.

15: Xu X, Lee KS. Characterization of the ATP-inhibited K+ current in canine coronary smooth muscle cells. Pflugers Arch. 1994 May;427(1-2):110-20. PubMed PMID: 8058459.

16: Baczkó I, Giles WR, Light PE. Pharmacological activation of plasma-membrane KATP channels reduces reoxygenation-induced Ca(2+) overload in cardiac myocytes via modulation of the diastolic membrane potential. Br J Pharmacol. 2004 Mar;141(6):1059-67. PubMed PMID: 14993099; PubMed Central PMCID: PMC1574274.

17: Zhang X, Zhang X, Xiong Y, Xu C, Liu X, Lin J, Mu G, Xu S, Liu W. Sarcolemmal ATP-sensitive potassium channel protects cardiac myocytes against lipopolysaccharide-induced apoptosis. Int J Mol Med. 2016 Sep;38(3):758-66. doi: 10.3892/ijmm.2016.2664. PubMed PMID: 27430376; PubMed Central PMCID: PMC4990318.

18: Xu X, Tsai TD, Lee KS. A specific activator of the ATP-inhibited K+ channels in guinea pig ventricular cells. J Pharmacol Exp Ther. 1993 Aug;266(2):978-84. PubMed PMID: 8394925.

19: Tai KK, McCrossan ZA, Abbott GW. Activation of mitochondrial ATP-sensitive potassium channels increases cell viability against rotenone-induced cell death. J Neurochem. 2003 Mar;84(5):1193-200. PubMed PMID: 12603842.

20: Suzuki M, Li RA, Miki T, Uemura H, Sakamoto N, Ohmoto-Sekine Y, Tamagawa M, Ogura T, Seino S, Marbán E, Nakaya H. Functional roles of cardiac and vascular ATP-sensitive potassium channels clarified by Kir6.2-knockout mice. Circ Res. 2001 Mar 30;88(6):570-7. PubMed PMID: 11282890.