HTL-9936 |
Catalog No.GC79297
One-Click Copy Product Info
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HTL-9936 is an orally active partial agonist of muscarinic M1 receptor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1438242-59-1
Sample solution is provided at 25 µL, 10mM.
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In Vivo, HTL-9936 (10-100 mg/kg; p.o.) induces transient, dose-dependent increases in heart rate and mean arterial blood pressure in adult male Wistar rats[6]. HTL-9936 (intravenous injection; 2-hour infusion) causes a transient, dose-dependent increase in blood pressure in purebred male Beagle dogs during intravenous infusion[6]. HTL-9936 (3 mg/kg) reverses scopolamine -induced cognitive impairment in rats, with an ED50 of 3 mg/kg[4]. HTL-9936 (10-100 mg/kg; i.p.) dose-dependently restores contextual fear conditioning impaired by Scopolamine in male C57BL/6J mice[6]. HTL-9936 (3-30 mg/kg; p.o.) dose-dependently reverses scopolamine-induced passive avoidance deficits in adult male Wistar rats[6]. HTL-9936 (3 mg/kg; p.o.) exerts an additive partial reversal effect on Scopolamine-induced passive avoidance deficits in adult male Wistar rats when combined with a sub-effective dose of Donepezil [6]. HTL-9936 (10 mg/kg; p.o.) improves working memory in the rat novel object recognition model. HTL-9936 (30 mg/kg; i.p.) improves fear conditioning learning and memory deficits in Tg37 mice, a prion disease model[6]. HTL-9936 (0.3-1 mg/kg, subcutaneous injection, once daily for 10 consecutive days) significantly improves visuospatial working memory in aged Beagle dogs[6]. HTL-9936 (0.3-3 mg/kg; subcutaneous injection) increases the δ wave power in resting-state electroencephalograms of adult male cynomolgus monkeys[6].
In Vitro, HTL-9936 (30 min) acts as a low-potency but high-efficacy partial agonist at native rat cortical M1 receptors, with an EC50 of 2-2.7 μM[1]. HTL-9936 (2 h) binds to human recombinant M1 receptor, with a Ki value of 9093 nM[1]. HTL-9936 potently stimulates calcium mobilization in CHO cells expressing human M1 receptors, with an EC50 of 168.8 nM[1]. HTL-9936 (10 min) stimulates the pERK signaling pathway in CHO cells expressing human M1 receptors, with an EC50 of 1161 nM[1]. HTL-9936 potently activates recombinant human M1 receptors (EC50 = 32 nM) and human M4 receptors (EC50 = 224 nM), but shows no activity against human M2 and M3 receptors[4].
References:
[1]. Broad LM, et al. Identification and pharmacological profile of SPP1, a potent, functionally selective and brain penetrant agonist at muscarinic M receptors. British journal of pharmacology. 2019 Jan;176(1):110-126.
[2]. Armer R, et al. Recent disclosures of clinical drug candidates. Drug News Perspect. 2006 Jan-Feb;19(1):65-72.
[3]. Nguyen HTM, et al. Opportunities and challenges for the development of M muscarinic receptor positive allosteric modulators in the treatment for neurocognitive deficits. British journal of pharmacology. 2024 Jul;181(14):2114-2142.
[4]. Felder CC, et al. Current status of muscarinic M1 and M4 receptors as drug targets for neurodegenerative diseases. Neuropharmacology. 2018 Jul 01;136(Pt C):449-458.
[5]. Johnson CR, et al. Drug Design Targeting the Muscarinic Receptors and the Implications in Central Nervous System Disorders. Biomedicines. 2022 Feb 07;10(2):398.
[6]. Brown AJH, et al. From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease. Cell. 2021 Nov 24;184(24):5886-5901.e22.
| Cas No. | 1438242-59-1 | SDF | |
| Formula | C20H35N3O3 | M.Wt | 365.51 |
| Solubility | Storage | Store at -20°C | |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7359 mL | 13.6795 mL | 27.359 mL |
| 5 mM | 547.2 μL | 2.7359 mL | 5.4718 mL |
| 10 mM | 273.6 μL | 1.368 mL | 2.7359 mL |
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)