Tolazoline
Based on 1 Customer Validation
Tolazoline (Imidaline) is an α-adrenergic receptor antagonist. Tolazoline inhibits Noradrenaline (HY-13715)-induced cell contraction, modulates vascular resistance, increases arterial pressure, and reverses bradycardia and tachypnea. Tolazoline can be used to study erectile dysfunction, α2-adrenergic receptor agonist-related poisoning, and skin vascular disease research.
For research use only. We do not sell to patients.
- Purity: 99.99%
- CAS No.: 59-98-3
- Formula: C10H12N2
- Molecular Weight:160.22
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
GPCR/G Protein Compound Library
HY-L006
-
Neuronal Signaling Compound Library
HY-L013
-
FDA-Approved Drug Library
HY-L022
-
Drug Repurposing Compound Library
HY-L035
-
Anti-Cardiovascular Disease Compound Library
HY-L046
-
Endocrinology Compound Library
HY-L047
-
Neurotransmitter Receptor Compound Library
HY-L062
-
Traditional Chinese Medicine Active Compound Library
HY-L065
-
FDA Approved & Pharmacopeial Drug Library
HY-L066
-
Anti-Alzheimer's Disease Compound Library
HY-L069
-
Neurodegenerative Disease-related Compound Library
HY-L086
-
Antidepressant Compound Library
HY-L108
-
Human Metabolite Library
HY-L123
-
Withdrawn Drug Compound Library
HY-L140
-
Off-patent Drug Library
HY-L141
-
Antihypertensive Compound Library
HY-L145
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
FDA-Approved Traditional Chinese Medicine Active Compound Library
HY-L163
-
Anti-Drug-Resistant Compound Library
HY-L169
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
FDA-Approved Drug Library Plus
HY-L022P
-
FDA-Approved Drug Library Mini
HY-L022M
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Mongolian Medicine Compound Library
HY-L238
-
Lactylation Compound Library
HY-L249
All Adrenergic Receptor Isoforms
More
Biological Activity
α-adrenoceptor.
Tolazoline (1 μM; 30 s) inhibits the Noradrenaline (HY-13715)-induced contraction of isolated smooth muscle cells from human corpus cavernosum[3].
Tolazoline inhibits the specific binding of 3H-DHE to smooth muscle cells from human corpus cavernosum with a lower affinity (IC50 = 0.1 μM)[3].
Tolazoline (10 nM-1 mM) dose-dependently reduces vascular resistance in isolated porcine perfused skin flaps precontracted with Norepinephrine (EC50 = 0.288 μM)[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Tolazoline (0.5 mg/kg; iv; injected into the femoral vein) causes an increase in arterial blood pressure in cats treated with Reserpine (HY-N0480) and anesthetized with Pentobarbitone sodium[6].
Tolazoline (2 mg/kg; i.v., once a week for 3 weeks) shortens the recumbency, head droop, reverses bradycardia and tachypnea in sheep treated with Xylazine[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 59-98-3
-
Appearance Solid
-
Molecular Weight 160.22
-
Formula C10H12N2
-
Color White to off-white
-
SMILES
C1(CC2=CC=CC=C2)=NCCN1
-
Synonyms
Imidaline; NSC35110
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 200 mg/mL (1248.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (31.21 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (31.21 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
-
Data Sheet (276 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
[1]. Megens AA, et al. Further validation of in vivo and in vitro pharmacological procedures for assessing the alpha 2/alpha 1-selectivity of test compounds: (1). Alpha-adrenoceptor antagonists. Eur J Pharmacol. 1986 Sep 23;129(1-2):49-55. [Content Brief]
[2]. Schwartz DD, et al. Selectivity of atipamezole, yohimbine and tolazoline for alpha-2 adrenergic receptor subtypes: implications for clinical reversal of alpha-2 adrenergic receptor mediated sedation in sheep. J Vet Pharmacol Ther. 1998 Oct;21(5):342-7. [Content Brief]
[3]. Costa P, et al. Adrenergic receptors on smooth muscle cells isolated from human penile corpus cavernosum. J Urol. 1993 Sep;150(3):859-63. [Content Brief]
[4]. Rogers RA, et al. Pharmacologic modulation of the cutaneous vasculature in the isolated perfused porcine skin flap. J Pharm Sci. 1994 Dec;83(12):1682-9. [Content Brief]
[5]. Lei L, et al. Activation of L-type calcium channel by tolazoline derivatives: role of isothiocyanate moiety. J Cardiovasc Pharmacol. 1998 May;31(5):721-33. [Content Brief]
[6]. BENFEY BG, et al. VASOCONSTRICTOR ACTION OF TOLAZOLINE. Br J Pharmacol Chemother. 1964 Feb;22(1):66-71. [Content Brief]
[7]. Hsu WH, et al. Effects of tolazoline and yohimbine on xylazine-induced central nervous system depression, bradycardia, and tachypnea in sheep. J Am Vet Med Assoc. 1987 Feb 15;190(4):423-6. [Content Brief]
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 | 6.2414 mL | 31.2071 mL | 62.4142 mL | 156.0355 mL |
| 5 mM | 1.2483 mL | 6.2414 mL | 12.4828 mL | 31.2071 mL | |
| 10 mM | 0.6241 mL | 3.1207 mL | 6.2414 mL | 15.6035 mL | |
| 15 mM | 0.4161 mL | 2.0805 mL | 4.1609 mL | 10.4024 mL | |
| 20 mM | 0.3121 mL | 1.5604 mL | 3.1207 mL | 7.8018 mL | |
| 25 mM | 0.2497 mL | 1.2483 mL | 2.4966 mL | 6.2414 mL | |
| 30 mM | 0.2080 mL | 1.0402 mL | 2.0805 mL | 5.2012 mL | |
| 40 mM | 0.1560 mL | 0.7802 mL | 1.5604 mL | 3.9009 mL | |
| 50 mM | 0.1248 mL | 0.6241 mL | 1.2483 mL | 3.1207 mL | |
| 60 mM | 0.1040 mL | 0.5201 mL | 1.0402 mL | 2.6006 mL | |
| 80 mM | 0.0780 mL | 0.3901 mL | 0.7802 mL | 1.9504 mL | |
| 100 mM | 0.0624 mL | 0.3121 mL | 0.6241 mL | 1.5604 mL |
Tolazoline Related Classifications
HY-A0066 Related Classifications
Powered by Bioz