1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. GABA Receptor
  3. rac-BHFF

rac-BHFF is a potent and orally active allosteric enhancer of GABAB receptor.

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

rac-BHFF Chemical Structure

rac-BHFF Chemical Structure

CAS No. : 123557-91-5

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5 mg USD 70 In-stock
10 mg USD 120 In-stock
25 mg USD 250 In-stock
50 mg USD 400 In-stock
100 mg USD 600 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

rac-BHFF is a potent and orally active allosteric enhancer of GABAB receptor[1].

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
1.9 μM
Compound: rac-BHFF
Agonist activity at human GABA-B B1/B2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 3 hrs by luciferase reporter gene assay
Agonist activity at human GABA-B B1/B2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 3 hrs by luciferase reporter gene assay
[PMID: 23428109]
In Vivo

rac-BHFF has anxiolytic-like properties in stress-induced hyperthermia (SIH) in mice[1].
rac-BHFF (3, 10, 30 and 100?mg/kg, p.o.) reverses SIH and high significance was reached for 100?mg?kg?1 (P<0.001)[1].

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

Animal Model: Male NMRI mice (20-25 g)[1].
Dosage: 3, 10, 30 or 100 mg/kg.
Administration: P.O..
Result: Significantly increased the LRR effects of a subthreshold dose of baclofen at doses of 3 mg/kg and above.
Molecular Weight

330.34

Formula

C17H21F3O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1OC2=C(C(C)(C)C)C=C(C(C)(C)C)C=C2C1(O)C(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (302.72 mM; ultrasonic and warming and heat to 60°C; 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 3.0272 mL 15.1359 mL 30.2718 mL
5 mM 0.6054 mL 3.0272 mL 6.0544 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 (protect from light). 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
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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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 (7.57 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 (7.57 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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
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 (protect from light). 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 3.0272 mL 15.1359 mL 30.2718 mL 75.6796 mL
5 mM 0.6054 mL 3.0272 mL 6.0544 mL 15.1359 mL
10 mM 0.3027 mL 1.5136 mL 3.0272 mL 7.5680 mL
15 mM 0.2018 mL 1.0091 mL 2.0181 mL 5.0453 mL
20 mM 0.1514 mL 0.7568 mL 1.5136 mL 3.7840 mL
25 mM 0.1211 mL 0.6054 mL 1.2109 mL 3.0272 mL
30 mM 0.1009 mL 0.5045 mL 1.0091 mL 2.5227 mL
40 mM 0.0757 mL 0.3784 mL 0.7568 mL 1.8920 mL
50 mM 0.0605 mL 0.3027 mL 0.6054 mL 1.5136 mL
60 mM 0.0505 mL 0.2523 mL 0.5045 mL 1.2613 mL
80 mM 0.0378 mL 0.1892 mL 0.3784 mL 0.9460 mL
100 mM 0.0303 mL 0.1514 mL 0.3027 mL 0.7568 mL
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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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rac-BHFF
Cat. No.:
HY-103519
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