DL-Thiorphan free base

Thiorphan is a selective neprilysin inhibitor.

For research use only. Not for human or veterinary use.

Target Neprilysin

Research area Neurological Disease

Purity >98% Stock Inquire

Data Sheet SDS COA

DL-Thiorphan structure

CAS No.: 76721-89-6

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 380.00	BP-02417-250mg	In stock	Get quote
500 mg	USD 610.00	BP-02417-500mg	In stock	Get quote
1 g	USD 970.00	BP-02417-1g	In stock	Get quote
2 g	USD 1,550.00	BP-02417-2g	In stock	Get quote
3 g	USD 1,870.00	BP-02417-3g	In stock	Get quote
5 g	USD 2,490.00	BP-02417-5g	In stock	Get quote
10 g	USD 3,980.00	BP-02417-10g	In stock	Get quote

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Description

Thiorphan is a selective neprilysin (NEP) inhibitor with an IC50 of 6.9 nM. Thiorphan competitively binds to NEP and blocks its activity, preventing the degradation of neuropeptides such as substance P (SP) and neurokinin NKA. In the field of neonatal brain injury research, Thiorphan can increase the levels of SP and NKA, activate NK1 and NK2 receptors and downstream transduction pathways, and inhibit excessive activation of NMDA receptors. Thus, Thiorphan can protect neocortical neurons from excitotoxic cell death. Thiorphan may also inhibit NEP from enhancing bronchoconstriction and can be used in the study of respiratory diseases .

Biological activity

In Vitro Thiorphan (5 μM; 12 h) protects neurons from excitotoxic stimulation and blocks the neurodegradation of substance P (10 μM) in primary neuronal cultures exposed to 300 μM NMDA. In Vivo Thiorphan (25 μg intracerebral or 50 mg/kg intraperitoneal; given as a single dose after ibotenic acid injection) reduces cortical damage and cortical caspase-3 cleavage in a mouse model of excitotoxic brain injury induced by ibotenic acid (HY-N2311), and this neuroprotective effect is still observed 12 hours after injury. This effect can be mimicked by substance P and neurokinin A, and is inhibited by NK1 and NK2 receptor blockers.

Identifiers

SMILES: SCC(C(NCC(O)=O)=O)CC1=CC=CC=C1
InChIKey: LJJKNPQAGWVLDQ-UHFFFAOYSA-N

Specifications

MW (average): 253.3170
Formula: C₁₂H₁₅NO₃S
CAS No.: 76721-89-6
Physical state: Solid
Color: White to off-white
Shipping: 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: Powder -20°C, protect from light

Solubility

Soluble in DMSO : 175 mg/mL

Documents

References

[1].Whyteside AR, et al. Human neprilysin-2 (NEP2) and NEP display distinct subcellular localisations and substrate preferences. FEBS Lett. 2008 Jul 9;582(16):2382-6.

[2]. Cheung D, et al. The effect of an inhaled neutral endopeptidase inhibitor, thiorphan, on airway responses to neurokinin A in normal humans in vivo. Am Rev Respir Dis. 1992 Jun;145(6):1275-80.

[3].Medja F, et al. Thiorphan, a neutral endopeptidase inhibitor used for diarrhoea, is neuroprotective in newborn mice. Brain. 2006 Dec;129(Pt 12):3209-23.

Same research area

Search Neurological Disease