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

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.

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PHA-543613

PHA-543613 構造式

CAS 番号 : 478149-53-0

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 148 在庫あり
Solution
10 mM * 1 mL in DMSO USD 148 在庫あり
Solid
5 mg $135 在庫あり
10 mg $220 在庫あり
25 mg $480 在庫あり
50 mg $820 在庫あり
100 mg $1300 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Other Forms of PHA-543613:

PHA-543613 関連抗体

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製品説明

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]
Cellular Effect
Cell Line Type Value Description References
SH-SY5Y IC50
>100 μM
Compound: 14, PHA-543613
Inhibition of alpha-3-beta-4 nAChR expressed in SHSY5Y cells by FLIPR assay
Inhibition of alpha-3-beta-4 nAChR expressed in SHSY5Y cells by FLIPR assay
[PMID: 16821801]
SH-SY5Y IC50
>100 μM
Compound: PHA-543613
Activity at alpha-3-beta-4 nACh receptor expressed in human SH-SY5Y cells by FLIPR assay
Activity at alpha-3-beta-4 nACh receptor expressed in human SH-SY5Y cells by FLIPR assay
[PMID: 18490160]
TE-671 IC50
>100 μM
Compound: 14, PHA-543613
Inhibition of alpha-1-beta-1-gamma-delta nAChR expressed in TE671cells by FLIPR assay
Inhibition of alpha-1-beta-1-gamma-delta nAChR expressed in TE671cells by FLIPR assay
[PMID: 16821801]
TE-671 IC50
>100 μM
Compound: PHA-543613
Activity at alpha-1-beta-1-gamma-delta nACh receptor expressed in human TE671 cells by FLIPR assay
Activity at alpha-1-beta-1-gamma-delta nACh receptor expressed in human TE671 cells by FLIPR assay
[PMID: 18490160]
体内実験

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[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.
分子量

271.32

分子式

C15H17N3O2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

H2O : 100 mg/mL (368.57 mM; Need ultrasonic)

DMSO : ≥ 100 mg/mL (368.57 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6857 mL 18.4284 mL 36.8568 mL
5 mM 0.7371 mL 3.6857 mL 7.3714 mL
10 mM 0.3686 mL 1.8428 mL 3.6857 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

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体積 （開始）

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
純度とドキュメンテーション

純度: 99.95%

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

取扱説明書 (2659 KB)
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.6857 mL 18.4284 mL 36.8568 mL 92.1421 mL
5 mM 0.7371 mL 3.6857 mL 7.3714 mL 18.4284 mL
10 mM 0.3686 mL 1.8428 mL 3.6857 mL 9.2142 mL
15 mM 0.2457 mL 1.2286 mL 2.4571 mL 6.1428 mL
20 mM 0.1843 mL 0.9214 mL 1.8428 mL 4.6071 mL
25 mM 0.1474 mL 0.7371 mL 1.4743 mL 3.6857 mL
30 mM 0.1229 mL 0.6143 mL 1.2286 mL 3.0714 mL
40 mM 0.0921 mL 0.4607 mL 0.9214 mL 2.3036 mL
50 mM 0.0737 mL 0.3686 mL 0.7371 mL 1.8428 mL
60 mM 0.0614 mL 0.3071 mL 0.6143 mL 1.5357 mL
80 mM 0.0461 mL 0.2304 mL 0.4607 mL 1.1518 mL
100 mM 0.0369 mL 0.1843 mL 0.3686 mL 0.9214 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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PHA-543613 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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.

Keywords:

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

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