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.


Chemical Structure

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P-1075
CAS# 60559-98-0

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

Price and Availability

Size Price Availability Quantity
10.0mg USD 330.0 2 Weeks
50.0mg USD 990.0 2 Weeks
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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

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).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 231.3 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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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.

P-1075

10.0mg / USD 330.0