2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR
  4. PHA-543613

PHA-543613 

Cat. No.: HY-105670 Purity: 99.95%
COA Handling Instructions

PHA-543613 is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki of 8.8 nM. PHA-543613 displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. PHA-543613 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 Chemical Structure

PHA-543613 Chemical Structure

CAS No. : 478149-53-0

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Solution
10 mM * 1 mL in DMSO USD 148 In-stock
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10 mg USD 220 In-stock
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Based on 1 publication(s) in Google Scholar

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PHA-543613 Related Antibodies

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Description

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

IC50 & Target

Ki: 8.8 nM (α7 nAChR)[1]
In Vivo

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

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

271.31

Appearance

Solid

Formula

C15H17N3O2
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (921.46 mM; Need ultrasonic)

H2O : 100 mg/mL (368.58 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6858 mL 18.4291 mL 36.8582 mL
5 mM 0.7372 mL 3.6858 mL 7.3716 mL
10 mM 0.3686 mL 1.8429 mL 3.6858 mL
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation

Purity: 99.95%

COA (249 KB) HNMR (249 KB) RP-HPLC (262 KB)

Handling Instructions (2659 KB)
References
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PHA-543613 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

PHA-543613478149-53-0PHA543613PHA 543613nAChRNicotinic acetylcholine receptorsOrally activebrain penetrantAlzheimer's diseaseschizophreniaInhibitorinhibitorinhibit

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