Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
SKU | Size | Availability | Price | Qty |
---|---|---|---|---|
D647537-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $160.90 | |
D647537-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $280.90 | |
D647537-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $610.90 | |
D647537-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,050.90 |
Specifications & Purity | ≥98% |
---|---|
Biochemical and Physiological Mechanisms | Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC 50 =110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC 50 =1.3 nM). Diprovocim activates downstream MAPK and NF-κB sign |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC 50 =110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC 50 =1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses In Vitro Diprovocim (5 nM in THP-1 and 500 nM in mouse peritoneal macrophage; 15-120 mins) induces phosphorylation of IKKα, IKKβ, p38, JNK, and ERK, as well as degradation of IκBα in THP-1 cells and mouse peritoneal macrophages. Diprovocim (0.01-10000 nM; 4 hours) induces dose-dependent TNF production by THP-1 cells (EC 50 =110 pM) and human peripheral blood mononuclear cells (PBMC) (EC 50 =875 pM) and by mouse peritoneal macrophages (EC 50 =1.3 nM) and bone marrow-derived dendritic cells (BMDC) (EC 50 =6.7 nM). In addition to TNF, Diprovocim induced IL-6 production by mouse BMDC. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: THP-1 cells and mouse peritoneal macrophages Concentration: 5 nM in THP-1 and 500 nM in mouse peritoneal macrophages Incubation Time: 15, 30, 60, 120 mins Result: Induced phosphorylation of IKKα, IKKβ, p38, JNK, and ERK, as well as degradation of IκBα. In Vivo Diprovocim (10 mg/kg) uses as an adjuvant and mixed with ovalbumin (OVA; 100 μg) by i.m. induces similar levels of serum OVA-specific IgG after 14 days. Diprovocim (10 mg/kg; i.m.) mixed with ovalbumin (OVA; 100 μg) before inoculation with B16-OVA cells immunizes significantly slows tumor growth rate but failed to prolong survival relative to OVA alone after 7 days. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: WT or Tlr2 −/− C57BL/6J miceDosage: 10 mg/kg Administration: IM Result: Induced similar levels of serum OVA-specific IgG, which were highly elevated compared with levels induced by immunization with OVA plus vehicle by i.m. with 100 μg OVA mixed with this drug. Form:Solid IC50& Target:TLR1|TLR2|p38 MAPK|NF-κB |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
IUPAC Name | (3S,4S)-1-[4-[(3S,4S)-3,4-bis[[(1S,2R)-2-phenylcyclopropyl]carbamoyl]pyrrolidine-1-carbonyl]benzoyl]-3-N,4-N-bis[(1S,2R)-2-phenylcyclopropyl]pyrrolidine-3,4-dicarboxamide |
---|---|
INCHI | InChI=1S/C56H56N6O6/c63-51(57-47-25-39(47)33-13-5-1-6-14-33)43-29-61(30-44(43)52(64)58-48-26-40(48)34-15-7-2-8-16-34)55(67)37-21-23-38(24-22-37)56(68)62-31-45(53(65)59-49-27-41(49)35-17-9-3-10-18-35)46(32-62)54(66)60-50-28-42(50)36-19-11-4-12-20-36/h1-24,39-50H,25-32H2,(H,57,63)(H,58,64)(H,59,65)(H,60,66)/t39-,40-,41-,42-,43-,44-,45-,46-,47+,48+,49+,50+/m1/s1 |
InChi Key | ABZBNXFGYUSVCJ-UYMKNZQYSA-N |
Canonical SMILES | C1C(C1NC(=O)C2CN(CC2C(=O)NC3CC3C4=CC=CC=C4)C(=O)C5=CC=C(C=C5)C(=O)N6CC(C(C6)C(=O)NC7CC7C8=CC=CC=C8)C(=O)NC9CC9C1=CC=CC=C1)C1=CC=CC=C1 |
Isomeric SMILES | C1[C@@H]([C@H]1NC(=O)[C@@H]2CN(C[C@H]2C(=O)N[C@H]3C[C@@H]3C4=CC=CC=C4)C(=O)C5=CC=C(C=C5)C(=O)N6C[C@H]([C@@H](C6)C(=O)N[C@H]7C[C@@H]7C8=CC=CC=C8)C(=O)N[C@H]9C[C@@H]9C1=CC=CC=C1)C1=CC=CC=C1 |
PubChem CID | 137553173 |
MeSH Entry Terms | (3R,4R)-1-(4-((3R,4R)-3,4-bis(((1R,2S)-2-phenylcyclopropyl)carbamoyl)pyrrolidine-1-carbonyl)benzoyl)-3-N,4-N-bis((1R,2S)-2-phenylcyclopropyl)pyrrolidine-3,4-dicarboxamide;diprovocim |
Molecular Weight | 909.08 |
Enter Lot Number to search for COA:
Solubility | DMSO : 33.33 mg/mL (36.66 mM; ultrasonic and warming and heat to 60°C) H2O : <0.1 mg/mL (ultrasonic) (insoluble) |
---|