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P1075

Names

[ CAS No. ]:
60559-98-0

[ Name ]:
P1075

[Synonym ]:
p-1075

Biological Activity

[Description]:

P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6), with an EC50 value of 45 nM for SUR2B-KIR6 channel activation[1]. P-1075 also P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts[2].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

[Target]

EC50: 45 nM (SUR2-KIR6)[1].


[References]

[1]. Schwanstecher M, et al. Potassium channel openers require ATP to bind to and act through sulfonylurea receptors. EMBO J. 1998 Oct 1;17(19):5529-35.

[2]. Oldenburg O, et al. P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts. J Mol Cell Cardiol. 2003 Sep;35(9):1035-42.

Chemical & Physical Properties

[ Density]:
1.07g/cm3

[ Boiling Point ]:
347.6ºC at 760 mmHg

[ Melting Point ]:
186-187 °C

[ Molecular Formula ]:
C12H17N5

[ Molecular Weight ]:
231.30

[ Flash Point ]:
164.1ºC

[ Exact Mass ]:
231.14800

[ PSA ]:
73.10000

[ LogP ]:
2.57268

[ Index of Refraction ]:
1.556

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
MF0175400
CHEMICAL NAME :
Guanidine, 2-cyano-1-tert-pentyl-3-(3-pyridyl)-
CAS REGISTRY NUMBER :
60559-98-0
LAST UPDATED :
199612
DATA ITEMS CITED :
2
MOLECULAR FORMULA :
C12-H17-N5
MOLECULAR WEIGHT :
231.34

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
14 mg/kg
TOXIC EFFECTS :
Vascular - BP lowering not characterized in autonomic section
REFERENCE :
JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 21,773,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>1 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 21,773,1978

Safety Information

[ Hazard Codes ]:
T+

[ HS Code ]:
2933399090

Customs

[ HS Code ]: 2933399090

[ Summary ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%


Related Compounds