PHA-543613 dihydrochloride

Cat. No.: HY-105670B: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PHA-543613 dihydrochloride is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a K_i value of 8.8 nM. PHA-543613 dihydrochloride displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. PHA-543613 dihydrochloride can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research.

For research use only. We do not sell to patients.

PHA-543613 dihydrochloride Chemical Structure

CAS No. : 478148-58-2

Size		Stock
MOQ		Minimum order quantity
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote
Other size		Get quote

Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other Forms of PHA-543613 dihydrochloride:

PHA-543613 Get quote
PHA-543613 hydrochloride Get quote

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

Description

PHA-543613 dihydrochloride is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a K_i value of 8.8 nM. PHA-543613 dihydrochloride displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors^[1]. PHA-543613 dihydrochloride can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research^[2]^[3].

IC₅₀ & Target

Ki: 8.8 nM (α7 nAChR)^[1]

In Vivo

PHA-543613 dihydrochloride (0.3 mg/kg) successfully reverses Scopolamine-induced short-term memory deficits in rats^[2].
PHA-543613 dihydrochloride (4 and 12 mg/kg; i.p. once) reduces behavioral deficits and brain edema is dependent on the PI3K-Akt signaling pathway^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male CD-1 mice with (intracerebral hemorrhage) ICH-induction or sham surgery^[3]
Dosage:	4 and 12 mg/kg
Administration:	Intraperitoneal injection; 4 and 12 mg/kg; 1 hour after surgery
Result:	Increased p-Akt and decreased p-GSK-3 and CC3 expressions in the ipsilateral hemisphere and reduced the neuronal cell death in the perihematomal area. Attenuated behavioral deficits and brain edema at 72 hours after ICH.

Molecular Weight

344.24

Formula

C₁₅H₁₉Cl₂N₃O₂

CAS No.

478148-58-2

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC2=C(OC=C2)C=N1)N[C@H]3CN4CCC3CC4.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Purity & Documentation

Purity: ≥99.0%

Select Batch:

Data Sheet (275 KB) SDS (252 KB)

COA (252 KB) Elemental Analysis Report (110 KB)

Handling Instructions (2659 KB)

References

[1]. Donn G Wishka, et al. Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship. J Med Chem. 2006 Jul 13;49(14):4425-36. [Content Brief]

[2]. Nóra Bruszt, et al. Potentiation of cognitive enhancer effects of Alzheimer's disease medication memantine by alpha7 nicotinic acetylcholine receptor agonist PHA-543613 in the Morris water maze task. Psychopharmacology (Berl). 2021 Nov;238(11):3273-3281. [Content Brief]

[3]. Krafft PR, et al. α7 nicotinic acetylcholine receptor agonism confers neuroprotection through GSK-3β inhibition in a mouse model of intracerebral hemorrhage. Stroke. 2012 Mar;43(3):844-50. [Content Brief]