HA 1100 hydrochloride

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Cat.No. 2415 - HA 1100 hydrochloride | C14H17N3O3S.HCl | CAS No. 155558-32-0
Description: Cell-permeable, selective Rho-kinase inhibitor
Alternative Names: Hydroxyfasudil
Chemical Name: 1-[(1,2-Dihydro-1-oxo-5-isoquinolinyl)sulfonyl]hexahydro-1H-1,4-diazepine hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (2)
Reviews
Literature (6)

Biological Activity

Cell-permeable active metabolite of Fasudil (HA 1077; Cat. No. 0541). Produces ATP-competitive and reversible inhibition of Rho-kinase and is ~ 100-fold selective over a range of other protein kinases. Inhibits neutrophil migration and produces potent vasodilatory effects in vivo.

Technical Data

M. Wt 343.83
Formula C14H17N3O3S.HCl
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 155558-32-0
PubChem ID 11371328
InChI Key XWWFOUVDVJGNNG-UHFFFAOYSA-N
Smiles Cl.OC1=NC=CC2=C(C=CC=C12)S(=O)(=O)N1CCCNCC1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 6.88 20

Preparing Stock Solutions

The following data is based on the product molecular weight 343.83. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 14.54 mL 72.71 mL 145.42 mL
1 mM 2.91 mL 14.54 mL 29.08 mL
2 mM 1.45 mL 7.27 mL 14.54 mL
10 mM 0.29 mL 1.45 mL 2.91 mL

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References

References are publications that support the biological activity of the product.

Arai et al (1993) Inhibition by the protein kinase inhibitor HA1077 of the activation of NADPH oxidase in human neutrophils. Biochem.Pharmacol. 46 1487 PMID: 8240400

Shimokawa et al (1999) Rho-kinase-mediated pathway induces enhanced myosin light chain phosphorylations in a swine model of coronary artery spasm. Cardiovasc.Res. 43 1029 PMID: 10615430

Utsunomiya et al (2001) Antianginal effects of hydroxyfasudil, a Rho-kinase inhibitor, in a canine model of effort angina. Br.J.Pharmacol. 134 1724 PMID: 11739249


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2 Citations for HA 1100 hydrochloride

Citations are publications that use Tocris products. Selected citations for HA 1100 hydrochloride include:

Kirschstein et al (2014) Age-dependent contribution of Rho kinase in CB-induced contraction of human detrusor smooth muscle in vitro. Acta Pharmacol Sin 35 74 PMID: 24122009

Pearn et al (2012) PropF. neurotoxicity is mediated by p75 neurotrophin receptor activation. Anesthesiology 116 352 PMID: 22198221


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


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