368874-34-4
368874-34-4 structure
- Name: TC14012
- Chemical Name: tc 14012
- CAS Number: 368874-34-4
- Molecular Formula: C90H140N34O19S2
- Molecular Weight: 2066.421
- Catalog: Signaling Pathways Anti-infection HIV
- Create Date: 2016-07-30 13:11:47
- Modify Date: 2024-01-14 09:36:02
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TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic inverse CXCR4 agonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity[1][2].
| Name | tc 14012 |
|---|---|
| Synonyms |
L-Arginyl-L-arginyl-N-[(3S,6S,9R,12R,17R,20S,23S,26S,29S,34aS)-26-(4-aminobutyl)-12-{[(2S)-1-amino-5-carbamimidamido-1-oxo-2-pentanyl]carbamoyl}-6-(3-carbamimidamidopropyl)-9,23,29-tris[3-(carbamoylamino)propyl]-3,20-bis(4-hydroxybenzyl)-1,4,7,10,18,21,24,27,30-nonaoxotriacontahydro-1H,16H-pyrrolo[2,1-p][1,2,5,8,11,14,17,20,23,26,29]dithianonaazacyclodotriacontin-17-yl]-3-(2-naphthyl)-L-alaninamide
L-Alaninamide, L-arginyl-L-arginyl-N-[(3S,6S,9R,12R,17R,20S,23S,26S,29S,34aS)-26-(4-aminobutyl)-12-[[[(1S)-1-(aminocarbonyl)-4-[(aminoiminomethyl)amino]butyl]amino]carbonyl]-9,23,29-tris[3-[(aminocarbonyl)amino]propyl]-6-[3-[(aminoiminomethyl)amino]propyl]triacontahydro-3,20-bis[(4-hydroxyphenyl)methyl]-1,4,7,10,18,21,24,27,30-nonaoxo-1H,16H-pyrrolo[2,1-p][1,2,5,8,11,14,17,20,23,26,29]dithianonaazacyclodotriacontin-17-yl]-3-(2-naphthalenyl) |
| Description | TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic inverse CXCR4 agonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity[1][2]. |
|---|---|
| Related Catalog | |
| Target |
CXCR4:19.3 nM (IC50) CXCR7:350 nM (EC50) HIV |
| In Vitro | TC14012 (1 mM) inhibits by more than 95% the infection of the CXCR4-expressing cells by the HXB2 (X4) or 89.6 (dual-tropic) strain whereas TC14012 (1 mM) does not inhibit at all the infection of the CCR5-expressing cells by the SF162 (R5) or 89.6 (dualtropic) strain[1]. TC14012 leads to erk 1/2 phosphorylation in U373 cells, which express endogenous CXCR7 but not CXCR4 in U373 cells. Upon stimulation with TC14012, CXCR7 and the CXCR7-Cter4 chimera are able to recruit arrestin, whereas CXCR4 and CXCR4-Cter7 remain silent[2]. |
| References |
| Density | 1.6±0.1 g/cm3 |
|---|---|
| Molecular Formula | C90H140N34O19S2 |
| Molecular Weight | 2066.421 |
| Exact Mass | 2065.047607 |
| PSA | 968.66000 |
| LogP | -9.27 |
| Index of Refraction | 1.715 |