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  4. Yohimbine Hydrochloride

Yohimbine hydrochloride is an alpha-2 renal adenomatase receptor inhibitor, blocking pre- and post-contact alpha-2 renal adenomatase receptors, causing the release of renal adenoma and multiple sclerosis.

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

Yohimbine Hydrochloride Chemical Structure

Yohimbine Hydrochloride Chemical Structure

CAS No. : 65-19-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
500 mg In-stock
1 g In-stock
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10 g   Get quote  

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Based on 11 publication(s) in Google Scholar

Other Forms of Yohimbine Hydrochloride:

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Description

Yohimbine hydrochloride is an alpha-2 renal adenomatase receptor inhibitor, blocking pre- and post-contact alpha-2 renal adenomatase receptors, causing the release of renal adenoma and multiple sclerosis.

Cellular Effect
Cell Line Type Value Description References
Sf9 IC50
3.67 nM
Compound: Yohimbine Hydrochloride
Displacement of [3H]MK9112 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells after 60 mins
Displacement of [3H]MK9112 from human recombinant adrenergic alpha2A receptor expressed in insect Sf9 cells after 60 mins
[PMID: 19788200]
In Vivo

Yohimbine Hydrochloride can be used in animal modeling to create hypertension models. Administering yohimbine hydrochloride (0.2 mg/kg, intraperitoneally) to rats 1 hour before stress each day for 14 consecutive days, followed by immersing the rats in cold water, significantly reduces sexual arousal and libido, as evidenced by increased latency and intervals. Reduced mating activity can be confirmed by decreased levels of testosterone, luteinizing hormone (LH), and follicle-stimulating hormone (FSH), along with a decline in testicular cholesterol content in the rats. Treatment with yohimbine significantly enhances sexual arousal and performance and corrects the impact of stress on mating behavior in male rats[1].

Induction of hypertension[1].
Background
The responses to pressor nerve stimulation in the pithed rat are mediated by α1A-, α2A- and α1D-adrenoceptors. Yohimbine (Hydrochloride), in addition to has antagonist actions as an α2A-adrenoceptor antagonist, has antagonist actions at α1D- and α1A-adrenoceptors against pressor responses[1].
Specific Mmodeling Methods
Rats: Wistar• male• 2-3 month old• weighing 250-350 g[1]
Administration: 1 mg/kg• i.v.• a single dose for 5 min[1]
Rat: SHRs and WKY• male• 20-week-old• weighing 300-350 g[4]
Administration: 2 mg/kg• i.p.• daily for 2 weeks[4]
Note
(1) Rats were pithed and ventilated with 100% O2 at a stroke rate of 60 per min and volume of approximately 0.67 mL/100 g. The carotid artery was cannulated for measurement of blood pressure and drugs were injected into the jugular vein[1].
(2) Yohimbine (Hydrochloride) was dissolved in distilled water and dilutions made up in normal saline (NaCl 0.9%)[1].
(3) Before administration, animals were housed four per cage with free access to water and standard laboratory rat chow (Purina). The colony room had a temperature of 24±1°C, humidity of 45-55% and light/dark cycle (lights on 07:00-19:00)[4].
Modeling Indicators
Molecular changes: Yohimbine (Hydrochloride) produced a significant 3-fold shift in pressor potency of Amidephrine (HY-136474) and significantly shifted the pressor responses to phenylephrine[1].
Blood pressure change: Yohimbine (Hydrochloride) reduced significantly the heart rate in spontaneously hypertensive rats (SHRs)[4].
Pathological changes: Yohimbine (Hydrochloride) elicited a marked, significant increase in receptor density over the outer strip of the outer medulla[4].
Correlated Product(s): Methoxy-idazoxan; BMY 7378 (HY-100554); Prazosin (HY-B0193); RS 100329 (HY-116379); ARC 239 (HY-12709); SK&F 86466
Opposite Product(s): Amidephrine (HY-136474); Clonidine (HY-12721)

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

Clinical Trial
Molecular Weight

390.90

Formula

C21H27ClN2O3

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

[H][C@]12C(NC3=C4C=CC=C3)=C4CCN1C[C@@]5(CC[C@H](O)[C@H](C(OC)=O)[C@]5(C2)[H])[H].[H]Cl

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 8.75 mg/mL (22.38 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)

H2O : 3.33 mg/mL (8.52 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5582 mL 12.7910 mL 25.5820 mL
5 mM 0.5116 mL 2.5582 mL 5.1164 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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* 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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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)

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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 (6.40 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 (6.40 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, 1 year; -20°C, 6 months (sealed storage, away from moisture)

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: 99.91%

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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.5582 mL 12.7910 mL 25.5820 mL 63.9550 mL
5 mM 0.5116 mL 2.5582 mL 5.1164 mL 12.7910 mL
DMSO 10 mM 0.2558 mL 1.2791 mL 2.5582 mL 6.3955 mL
15 mM 0.1705 mL 0.8527 mL 1.7055 mL 4.2637 mL
20 mM 0.1279 mL 0.6395 mL 1.2791 mL 3.1977 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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    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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Yohimbine Hydrochloride
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