| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
KZR-8445 (0.1-10000 nM; 24 hours) directly targets Sec61α and can effectively inhibit the secretion of IL-2-GLuc and TNFα-GLuc in HEK293 Flp-In T-REx cells expressing wild-type Sec61α, with an IC50 value of approximately 100 nM [1]. KZR-8445 (24 hours) can inhibit the secretion of GLuc reporter genes fused with HER3, prolactin, PD1, TNFα and IL-2 signal peptides in HEK293 Flp-In T-REx cells, with an IC50 value ranging from 32 nM to 1068 nM [1]. KZR-8445 can effectively inhibit the secretion of Sec61-dependent pro-inflammatory cytokines in activated human peripheral blood mononuclear cells (PBMCs), with an IC50 value below micromolar and maintaining cell viability even at concentrations up to 20 µM [1]. KZR-8445 (0.01-10 µM; 2 hours) can inhibit the replication of SARS-CoV-2 and the biosynthesis of spike protein in Vero E6 cells, and can maintain cell viability of more than 50% even at concentrations up to 10 µM [1].
|
|---|---|
| ln Vivo |
KZR-8445 (10–20 mg/kg; intravenous injection; three times a week/once a week; 2 weeks) dose-dependently blocked disease progression in a mouse model of rheumatoid arthritis [1].
|
| Animal Protocol |
Animal/Disease Models:BALB/c (female, 7-8 weeks old, intravenous injection of anti-type II collagen antibody mixture on day 0, intraperitoneal injection of LPS to induce rheumatoid arthritis on day 3) [1]
Doses: 10 mg/kg; 20 mg/kg Route of Administration: Intravenous injection; once a week; for 2 weeks Experimental Results: Three times a week, doses of 10 mg/kg and 20 mg/kg significantly inhibited disease progression. A dose of 20 mg/kg once a week also significantly inhibited disease progression. All treatment groups showed similar or greater changes in body weight as the vector control mice, and no obvious toxicity was observed. |
| References |
| Molecular Formula |
C49H61BRF6N8O8
|
|---|---|
| Molecular Weight |
1083.95
|
| CAS # |
2377734-91-1
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
BrC(C=C1)=CC=C1CN2C3=CC=CC=C3C(C[C@@H]4N(C([C@@H](NC([C@@H](N(C([C@@H](NC([C@H](OC([C@@H](N(C([C@@H](NC4=O)CC(C)C)=O)C)C)=O)CCC#N)=O)CC(F)(F)F)=O)C)CC(C)C)=O)CC(F)(F)F)=O)C)=C2
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 0.9226 mL | 4.6128 mL | 9.2255 mL | |
| 5 mM | 0.1845 mL | 0.9226 mL | 1.8451 mL | |
| 10 mM | 0.0923 mL | 0.4613 mL | 0.9226 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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