| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
Tildacerfont targets the corticotropin-releasing factor type 1 (CRF1) receptor, a key regulator of the hypothalamic-pituitary-adrenal (HPA) axis. By antagonizing this receptor, it reduces the secretion of ACTH from the pituitary gland, which in turn decreases the production of adrenal androgens. This mechanism is beneficial for treating conditions like congenital adrenal hyperplasia, where excess ACTH drives androgen overproduction.
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| ln Vitro |
Tildacerfont is a potent CRF1 receptor antagonist. It effectively reduces ACTH and adrenal androgen levels. It has good safety and is a selective antagonist. Its in vitro activity is characterized by high affinity and potency at the CRF1 receptor. In HepG2 cells, it has EC50 values of 0.65 pM and 3 nM for PPARα and PPARγ, respectively.
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| ln Vivo |
Tildacerfont has been studied in preclinical models and clinical trials for the treatment of congenital adrenal hyperplasia (CAH). It effectively reduces ACTH and adrenal androgen levels in vivo. Its safety and efficacy have been evaluated in clinical studies for CAH and other conditions characterized by elevated ACTH. It is a promising therapeutic agent for managing CAH.
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| Enzyme Assay |
In vitro receptor binding assays for Tildacerfont measure its affinity for the CRF1 receptor. The receptor is incubated with a radiolabeled ligand and varying concentrations of the compound, and displacement is measured to determine binding affinity (Ki). Functional assays assess its antagonist activity by measuring CRF-induced cAMP accumulation in cells expressing the receptor.
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| Cell Assay |
In vitro cellular assays for Tildacerfont involve treating cells expressing the CRF1 receptor with the compound and measuring its ability to block CRF-induced signaling. Its effects on ACTH secretion can be studied in pituitary cell cultures. Its effects on adrenal androgen production can be assessed in adrenal cell cultures. Its cytotoxicity and cell viability are also evaluated.
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| Animal Protocol |
In vivo animal models for Tildacerfont include rodent models of congenital adrenal hyperplasia or stress-induced HPA axis activation to evaluate its effects on ACTH and adrenal androgen levels. Animals are treated with the compound, and hormone levels are measured in blood. Its effects on behavior and stress responses are also studied.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Tildacerfont indicate that it is orally active. It is well-absorbed after oral administration and has good bioavailability. It is metabolized in the liver, and its metabolites are excreted in urine and feces. Its half-life is consistent with once- or twice-daily dosing. Its pharmacokinetics have been characterized in preclinical and clinical studies.
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| Toxicity/Toxicokinetics |
Tildacerfont is generally well-tolerated in clinical studies. Common side effects may include gastrointestinal disturbances, headache, and fatigue. As a CRF1 antagonist, it may have effects on the HPA axis and stress responses. Its long-term safety is being evaluated in clinical trials. It has shown good safety in studies for CAH.
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| References | |
| Additional Infomation |
Tildacerfont is a potent and orally active CRF1 receptor antagonist that reduces ACTH and adrenal androgen levels. It has been investigated for the treatment of congenital adrenal hyperplasia (CAH). It has good safety and is a selective CRF1 antagonist. It has been studied in clinical trials for CAH and other conditions characterized by elevated ACTH.
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| Molecular Formula |
C20H26CLN5OS
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|---|---|
| Molecular Weight |
419.971341609955
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| Exact Mass |
419.154
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| CAS # |
1014983-00-6
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.681
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| LogP |
2.65
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| InChi Key |
XVAWSBAQNIXMIO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H26ClN5OS/c1-5-14(6-2)15-11-12(3)22-19-16(13(4)24-26(15)19)17-18(21)23-20(28-17)25-7-9-27-10-8-25/h11,14H,5-10H2,1-4H3
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| Chemical Name |
4-[4-chloro-5-(2,5-dimethyl-7-pentan-3-ylpyrazolo[1,5-a]pyrimidin-3-yl)-1,3-thiazol-2-yl]morpholine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~10 mg/mL (~23.81 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3811 mL | 11.9056 mL | 23.8112 mL | |
| 5 mM | 0.4762 mL | 2.3811 mL | 4.7622 mL | |
| 10 mM | 0.2381 mL | 1.1906 mL | 2.3811 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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