1-amino-8-naphthol-2,4-disulfonic acid monosodium salt

Names

[ Name ]:
1-amino-8-naphthol-2,4-disulfonic acid monosodium salt

[Synonym ]:
1-AMINO-8-NAPHTHOL-2,4-DISULFONIC ACID MONOSODIUM SALT
MFCD00068275
Chicago Acid Hydrate
SS Acid Hydrate
Sodium Hydrogen 4-Amino-5-hydroxy-1,3-naphthalenedisulfonate Hydrate
Monosodium 1-Amino-8-naphthol-2,4-disulfonate Hydrate
EINECS 258-185-0
4-Amino-5-hydroxy-1,3-naphthalenedisulfonic Acid Monosodium Salt Hydrate
2S Acid Hydrate

Biological Activity

[Description]:

CaMKP inhibitor sodium is a selective inhibitor of ROCK1 with an IC50 value of 14 nM.

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> ROCK

Signaling Pathways >> Stem Cell/Wnt >> ROCK

Signaling Pathways >> TGF-beta/Smad >> ROCK

[Target]

IC50: 14 nM (ROCK1)[1].

[In Vitro]

CaMKP inhibitor sodium at 1 μM reduces ROCK2 activity over 20-fold, under conditions in which the only other kinase tested that is significantly inhibited is MSK1 whose activity is reduced ~5-fold. CaMKP inhibitor sodium is a more selective ROCK2 inhibitor than the widely utilized ROCK inhibitor Y-27632 as assessed on kinase-specificity panel, and does not significantly inhibit LRRK2 even at doses as high as 30 μM (500-fold higher than IC50 of inhibition of ROCK2). CaMKP inhibitor sodium slightly inhibits RSK and p70S6K with IC50 of 0.78 μM and 1.94 μM, respectively. CaMKP inhibitor sodium significantly inhibits rat aortic ring dilation with IC50 of 190 nM[2].

[In Vivo]

CaMKP inhibitor sodium has 61% oral bioavailability in male Sprague-Dawley rats. Oral administration of CaMKP inhibitor sodium at single doses of 3-30 mg/kg dramatically reduces mean arterial pressure in the spontaneously hypertensive rats (SHRs) in a dose-dependent manner, with a maximum decrease of 50 mmHg after approximately 2 hours treatment at dose of 30 mg/kg[1].

[References]

[1]. Goodman KB et al Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors. J Med Chem. 2007 Jan 11;50(1):6-9.

[2]. Nichols RJ et al Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease. Biochem J. 2009 Oct 23;424(1):47-60.

Chemical & Physical Properties

[ Density]:
1.477 g/mL at 25 °C(lit.)

[ Boiling Point ]:
270-272 °C(lit.)

[ Melting Point ]:
12-16 °C(lit.)

[ Molecular Formula ]:
C₁₀H₈NNaO₇S₂

[ Molecular Weight ]:
341.29

[ Flash Point ]:
>230 °F

[ Exact Mass ]:
340.96400

[ PSA ]:
174.58000

[ LogP ]:
3.02120

[ Index of Refraction ]:
n20/D 1.498(lit.)

MSDS

Click to get detail MSDS

Safety Information

[ Safety Phrases ]:
S22-S24/25

[ HS Code ]:
2922199090

Customs

[ HS Code ]: 2922199090

[ Summary ]:
2922199090. other amino-alcohols, other than those containing more than one kind of oxygen function, their ethers and esters; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%