Benserazide dot HCl (Ro 4-4602)An aromatic L-aminoacid decarboxylase inhibitor

Benserazide·HCl (Ro 4-4602) (CAS 14919-77-8)

BenserazideandmiddotHCl (Ro 4-4602) | CAS 14919-77-8 is rated 5.0 out of 5 by 1.
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Synonym: DL-Serine 2-(2,3,4-trihydroxybenzyl)hydrazide hydrochloride
Application: An aromatic L-aminoacid decarboxylase inhibitor
CAS Number: 14919-77-8
Purity: ≥99%
Molecular Weight: 293.74
Molecular Formula: C10H15N3O5 HCl
* Refer to Certificate of Analysis for lot specific data (including water content).
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Benserazide·HCl (Ro 4-4602) is a small molecule inhibitor of extracerebral DDC (aromatic L-aminoacid decarboxylase), also known as DOPA decarboxylase. This protein is responsible for decarboxylating L-DOPA to dopamine, 5-hydroxytryptophan to serotonin, and tryptophan to tryptamine. L-DOPA is delivered directly to subjects suffering from a dopaminergic dysfunction such as in Parkinson's disease and dopamine-responsive dystonia - L-DOPA is the natural precursor to dopamine and freely passes the blood brain barrier, while dopamine itself does not. Inhibition of the extracerebral decarboxylation of L-DOPA into dopamine by Benserazide increases the availability of L-DOPA for movement into the brain and subsequent conversion to dopamine. Benserazide·HCl (Ro 4-4602) is an inhibitor of TH and TPH.


References

1. Pinder, R.M., et al. 1976. Drugs. 11: 329-377. PMID: 782834
2. Marion, M.H., et al. 1987. Adv Neurol. 45: 493-496. PMID: 3548262
3. Merims, D., et al. 2008. Parkinsonism Relat. Disord. 14: 273-280. PMID: 17988927

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in water (10 mg/ml), DMSO, and methanol. Insoluble in 100% ethanol, and acetone.
Storage :
Store at 4° C
Melting Point :
146-148° C
IC50 :
Estrogen receptor beta: IC50 = 30.54 µM (human); SUMO-activating enzyme subunit 2: IC50 = 23.18 µM (human); Intestinal alkaline phosphatase: IC50 = 50.9 µM (Mus musculus); SUMO-activating enzyme subunit 1: IC50 = 1.66 µM (human); SUMO-activating enzyme subunit 2: IC50 = 1.66 µM (human); Zinc finger protein mex-5: EC5050 = 112 nM (Caenorhabditis elegans); Intestinal alkaline phosphatase: EC5050 = 5470 nM (human)
pK Values :
pKa: 9.4, pKb: 6.72
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
2
RTECS :
VT9632300
PubChem CID :
26964
Merck Index :
14: 1050
MDL Number :
MFCD00078571
EC Number :
238-991-9
SMILES :
C1=CC(=C(C(=C1CNNC(=O)C(CO)N)O)O)O.Cl

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Kim Kim, BK. et al. (PubMed 26022398) reported that Benserazide is the first allosteric inhibitor of Coxsackievirus B3 3C protease. -SCBT Publication Review
Date published: 2015-07-18
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