H-20
Based on 1 publication(s) in Google Scholar
H-20 is a PD-1 agonist peptide. H-20 increases μOR mRNA in DRG neurons and modulates μOR-mediated analgesia. H-20 produces synergistic analgesic effects in inflammatory pain models and can reduce analgesic-induced tolerance, hyperalgesia, constipation, and motor impairment. H-20 can be used in pain-related research.
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- Pureté : 99.55%
- CAS No.: 3020015-02-2
- Formule: C44H64N10O15
- Masse moléculaire:973.04
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Stockage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) H-20
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Activité biologique
Description
IC50 & Target
[1]|
μ Opioid Receptor/MOR |
In Vivo
H-20 (7.64-15.26 nmol; i.t. or i.pl.) produces dose-dependent analgesia in acute inflammatory pain and synergistically enhances μ-opioid receptor agonist analgesia via the i.t. or i.pl. routes[1].
H-20 exhibited analgesic effects in the carrageenan-induced acute inflammatory pain model in mice; the intrathecal ED50 values were 14.89 nmol/mouse in male mice and 15.26 nmol/mouse in female mice; the plantar ED50 was 7.64 nmol/mouse[1].
H-20 administered in combination with μ-opioid receptor agonists produces synergistic analgesic effects in the carrageenan pain model and the complete Freund's adjuvant (CFA) (HY-153808)-induced chronic inflammatory pain model in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (wild-type naïve; male unless indicated)[1]
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Dosage:30 nmol; i.t.; twice‑daily; 3 days (μOR‑mRNA measurement).
30 nmol, or co‑administered with 0.1 nmol μ‑opioid receptor agonist; i.t.; twice‑daily; 7 days (baseline mechanical‑pain‑threshold assay).
30 nmol, or co‑administered with 0.1 nmol μ‑opioid receptor agonist; i.t.; twice‑daily; 5 days (gastrointestinal‑motility evaluation).
30 nmol, or co‑administered with 0.1 nmol μ‑opioid receptor agonist; i.t.; single injection (motor‑coordination test).
30 nmol, or co‑administered with 0.1 nmol μ‑opioid receptor agonist; i.t.; single injection (locomotor‑activity test). -
Administration:Administered i.t.; twice daily; 3 days (μOR‑mRNA measurement).
Administered i.t.; twice daily; 7 days (baseline mechanical‑pain‑threshold assay).
Administered i.t.; twice daily; 5 days (gastrointestinal‑motility evaluation).
Administered i.t.; single injection (motor‑coordination test).
Administered i.t.; single injection (locomotor‑activity test). -
Result:Elevated DRG μOR‑mRNA expression after 30 nmol intrathecal twice‑daily dosing for 3 days.
Maintained baseline mechanical paw‑withdrawal thresholds upon repeated 30 nmol monotherapy or 10 nmol co‑administration with 0.1 nmol μ‑opioid receptor agonist.
Diminished fecal boli counts under 20 nmol μ‑opioid receptor‑agonist monotherapy relative to saline or 30 nmol monotherapy.
Generated milder gastrointestinal‑function inhibition with 0.1 nmol μ‑opioid receptor‑agonist co‑administration versus 20 nmol agonist monotherapy.
Preserved mouse motor‑endurance time for 30 nmol monotherapy or 10 nmol co‑administration with 0.1 nmol μ‑opioid receptor agonist; provoked obvious 1‑h motor impairment by agonist‑only treatment.
Showed unchanged open‑field locomotor activity following 30 nmol intrathecal monotherapy compared with saline.
Lowered central‑to‑total activity‑distance ratio and produced circling‑type trajectories by 20 nmol intrathecal μ‑opioid receptor‑agonist monotherapy.
Slightly and non‑significantly reduced central‑to‑total activity‑distance ratio under 0.1 nmol μ‑opioid receptor‑agonist co‑administration, with trajectories comparable to saline group.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 3020015-02-2
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Appearance Solid
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Masse moléculaire 973.04
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Formule C44H64N10O15
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Color White to off-white
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Sequence
Ile-Ser-Tyr-Gly-Gly-Ala-Asp-Tyr-Lys
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Sequence Shortening
ISYGGADYK
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (102.77 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.57 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.57 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Protocole
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Formalin-Induced Paw Inflammation/Nociceptive Inflammation
The formalin-induced paw inflammation/nociceptive test is a chemical persistent pain model in rodents in which subcutaneous injection of formalin into the hind paw produces spontaneous nocifensive behaviors such as flinching and licking. The response is classically biphasic, consisting of an early acute phase (Phase I) reflecting direct activation of peripheral nociceptors (particularly C-fiber afferents), followed by a later prolonged phase (Phase II) associated with central sensitization in the spinal dorsal horn driven by sustained afferent input and inflammatory signaling. This model is widely used to evaluate analgesic and anti-inflammatory interventions because it captures both peripheral nociception and central sensitization processes within a single assay system.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 (sealed storage, away from moisture). 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 | 1.0277 mL | 5.1385 mL | 10.2771 mL | 25.6927 mL |
| 5 mM | 0.2055 mL | 1.0277 mL | 2.0554 mL | 5.1385 mL | |
| 10 mM | 0.1028 mL | 0.5139 mL | 1.0277 mL | 2.5693 mL | |
| 15 mM | 0.0685 mL | 0.3426 mL | 0.6851 mL | 1.7128 mL | |
| 20 mM | 0.0514 mL | 0.2569 mL | 0.5139 mL | 1.2846 mL | |
| 25 mM | 0.0411 mL | 0.2055 mL | 0.4111 mL | 1.0277 mL | |
| 30 mM | 0.0343 mL | 0.1713 mL | 0.3426 mL | 0.8564 mL | |
| 40 mM | 0.0257 mL | 0.1285 mL | 0.2569 mL | 0.6423 mL | |
| 50 mM | 0.0206 mL | 0.1028 mL | 0.2055 mL | 0.5139 mL | |
| 60 mM | 0.0171 mL | 0.0856 mL | 0.1713 mL | 0.4282 mL | |
| 80 mM | 0.0128 mL | 0.0642 mL | 0.1285 mL | 0.3212 mL | |
| 100 mM | 0.0103 mL | 0.0514 mL | 0.1028 mL | 0.2569 mL |
H-20 Related Classifications
HY-P10908 Related Classifications
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