2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. Picrotin

Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs with IC50 values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission.

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

Picrotin Chemical Structure

Picrotin Chemical Structure

CAS No. : 21416-53-5

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Based on 1 publication(s) in Google Scholar

Other Forms of Picrotin:

Picrotin Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs with IC50 values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission[1][2].

IC50 & Target

IC50: 13.1 μM (α2 GlyRs)[1]
In Vitro

Picrotin has sensitivity for α2 GlyRs with IC50 value of 13.1 μM[1].

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

Picrotin Related Antibodies
Molecular Weight

310.30

Formula

C15H18O7
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@]([C@@](C1)([C@]2([H])[C@@](C(O)(C)C)([H])[C@@]3([H])OC2=O)O)([C@]3([H])OC4=O)[C@@]54[C@@H]1O5
Structure Classification
Initial Source
Shipping

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

DMSO : 100 mg/mL (322.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2227 mL 16.1134 mL 32.2269 mL
5 mM 0.6445 mL 3.2227 mL 6.4454 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.

  • Molarity Calculator

  • Dilution Calculator

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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.06 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.06 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.92%

SDS (251 KB)

COA (261 KB) RP-HPLC (243 KB)

Handling Instructions (2659 KB)
References

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
DMSO 1 mM 3.2227 mL 16.1134 mL 32.2269 mL 80.5672 mL
5 mM 0.6445 mL 3.2227 mL 6.4454 mL 16.1134 mL
10 mM 0.3223 mL 1.6113 mL 3.2227 mL 8.0567 mL
15 mM 0.2148 mL 1.0742 mL 2.1485 mL 5.3711 mL
20 mM 0.1611 mL 0.8057 mL 1.6113 mL 4.0284 mL
25 mM 0.1289 mL 0.6445 mL 1.2891 mL 3.2227 mL
30 mM 0.1074 mL 0.5371 mL 1.0742 mL 2.6856 mL
40 mM 0.0806 mL 0.4028 mL 0.8057 mL 2.0142 mL
50 mM 0.0645 mL 0.3223 mL 0.6445 mL 1.6113 mL
60 mM 0.0537 mL 0.2686 mL 0.5371 mL 1.3428 mL
80 mM 0.0403 mL 0.2014 mL 0.4028 mL 1.0071 mL
100 mM 0.0322 mL 0.1611 mL 0.3223 mL 0.8057 mL
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Picrotin 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:

Picrotin21416-53-5GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorpicrotoxinGABAA receptors (GABAARs)glycine receptors (GlyRs)central nervous systemneurotransmissionInhibitorinhibitorinhibit

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