2. Membrane Transporter/Ion Channel
  3. Potassium Channel
  4. Apamin

Apamin (Apamine) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca2+-activated K+ (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity.

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Kundenspezifische Peptidsynthese

Apamin

Apamin Chemische Struktur

CAS. Nr. : 24345-16-2

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Based on 10 publication(s) in Google Scholar

Other Forms of Apamin:

Apamin Related Antibodies

Top Publications Citing Use of Products

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Beschreibung

Apamin (Apamine) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca2+-activated K+ (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity[1].

IC50 & Target

K+ channel[1]
Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.16 1
Compound: 14
Inhibition of Kca2.3 channel expressed in HEK293 cells by thallium flux assay
Inhibition of Kca2.3 channel expressed in HEK293 cells by thallium flux assay
[PMID: 18774291]
HEK293 IC50
0.00016 3
Compound: 14
Inhibition of Kca2.3 channel expressed in HEK293 cells by thallium flux assay
Inhibition of Kca2.3 channel expressed in HEK293 cells by thallium flux assay
[PMID: 18774291]
HEK293 IC50
0.00016 3
Compound: apamin
Inhibition of Kca2.3 channel expressed in HEK293 cells by thallium flux assay
Inhibition of Kca2.3 channel expressed in HEK293 cells by thallium flux assay
[PMID: 18824351]
HEK293 IC50
0.16 1
Compound: apamin
Inhibition of Kca2.3 channel expressed in HEK293 cells by thallium flux assay
Inhibition of Kca2.3 channel expressed in HEK293 cells by thallium flux assay
[PMID: 18824351]
HEK293 IC50
uM 3
Compound: 14
Inhibition of Kca2.3 channel expressed in HEK293 cells by electrophysiology assay
Inhibition of Kca2.3 channel expressed in HEK293 cells by electrophysiology assay
[PMID: 18774291]
HEK293 IC50
0.000064 3
Compound: 14
Inhibition of Kca2.3 channel expressed in HEK293 cells by electrophysiology assay
Inhibition of Kca2.3 channel expressed in HEK293 cells by electrophysiology assay
[PMID: 18774291]
HEK293 IC50
uM 3
Compound: apamin
Inhibition of Kca2.3 channel expressed in HEK293 cells by electrophysiology assay
Inhibition of Kca2.3 channel expressed in HEK293 cells by electrophysiology assay
[PMID: 18824351]
HEK293 IC50
0.000064 3
Compound: apamin
Inhibition of Kca2.3 channel expressed in HEK293 cells by electrophysiology assay
Inhibition of Kca2.3 channel expressed in HEK293 cells by electrophysiology assay
[PMID: 18824351]
Hepatocyte IC50
0.001 3
Compound: 1 Apamin
Inhibition of apamin-sensitive SKCa channel of guinea-pig hepatocytes
Inhibition of apamin-sensitive SKCa channel of guinea-pig hepatocytes
[PMID: 15225721]
Hepatocyte IC50
0.001 3
Compound: 1 Apamin
Inhibition of apamin-sensitive SKCa channel of guinea-pig hepatocytes
Inhibition of apamin-sensitive SKCa channel of guinea-pig hepatocytes
[PMID: 15225721]
In Vitro

Apamin (0.5-2 μg/mL; 24 hours; HSC-T6 cells) treatment markedly reduces the expression of α-SMA in the TGF-β1-induced HSC-T6 cells. Apamin treatment abrogats the activation of p-Smad2/3 and Smad4 induced by TGF-β1[1].

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

Apamin Related Antibodies

Western Blot Analysis[1]

Cell Line: HSC-T6 cells
Concentration: 0.5 µg/mL, 1 µg/mL and 2 µg/mL
Incubation Time: 24 hours
Result: Markedly reduced the expression of α-SMA in the TGF-β1-induced HSC-T6 cells. Abrogated the activation of p-Smad2/3 and Smad4 induced by TGF-β1.
In Vivo

Apamin (0.1 mg/kg; intraperitoneal injection; twice a week; for 4 weeks; C57BL/6 male mice) treatment results in decreased liver injury and proinflammatory cytokine levels. Apamin suppresses the deposition of collagen, proliferation of BECs and expression of fibrogenic genes in the 3,5-diethoxycarbonyl-1,4-dihydrocollidine (DDC)-fed mice[1].

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

Animal Model: 8-week-old C57BL/6 male mice (20-25 g) with DDC feeding[1]
Dosage: 0.1 mg/kg
Administration: Intraperitoneal injection; twice a week; for 4 weeks
Result: Resulted in decreased liver injury and proinflammatory cytokine levels. Suppressed the deposition of collagen, proliferation of BECs and expression of fibrogenic genes in the DDC-fed mice.
Molekulargewicht

2027.34

Formel

C79H131N31O24S4
CAS. Nr.
Appearance

Solid

Color

White to off-white

Sequence

Cys-Asn-Cys-Lys-Ala-Pro-Glu-Thr-Ala-Leu-Cys-Ala-Arg-Arg-Cys-Gln-Gln-His-NH2 (Disulfide bridge: Cys1-Cys11;Cys3-Cys15)
Sequence Shortening

CNCKAPETALCARRCQQH-NH2 (Disulfide bridge: Cys1-Cys11;Cys3-Cys15)
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

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

Lösungsmittel & Löslichkeit
In Vitro: 

H2O : 100 mg/mL (49.33 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.4933 mL 2.4663 mL 4.9326 mL
5 mM 0.0987 mL 0.4933 mL 0.9865 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 (sealed storage, away from moisture). 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.

  • Molaritätsrechner

  • Verdünnungsrechner

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

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).
Reinheit & Dokumentation
Verweise

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 (sealed storage, away from moisture). 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 1 mM 0.4933 mL 2.4663 mL 4.9326 mL 12.3314 mL
5 mM 0.0987 mL 0.4933 mL 0.9865 mL 2.4663 mL
10 mM 0.0493 mL 0.2466 mL 0.4933 mL 1.2331 mL
15 mM 0.0329 mL 0.1644 mL 0.3288 mL 0.8221 mL
20 mM 0.0247 mL 0.1233 mL 0.2466 mL 0.6166 mL
25 mM 0.0197 mL 0.0987 mL 0.1973 mL 0.4933 mL
30 mM 0.0164 mL 0.0822 mL 0.1644 mL 0.4110 mL
40 mM 0.0123 mL 0.0617 mL 0.1233 mL 0.3083 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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Apamin 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.

Keywords:

Apamin24345-16-2ApaminePotassium ChannelKcsAInhibitorinhibitorinhibit

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