A peptide inhibitor of ACE2
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DX600 (trifluoroacetate salt)

Item No. 22186

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Molecular Formula
C141H187N35O40S2 • XCF3COOH
Formula Weight
3076.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:6): 0.13 mg/mlEthanol: slightly soluble
λmax
221, 280 nm
SMILES
NC(CNC(CNC(CNC([C@H](CCC(O)=O)NC([C@@H]1CCCN1C([C@@H](NC([C@@H]2CCCN2C([C@@H](NC([C@@]([C@@H](C)O)([H])NC([C@@H](NC([C@H](CCCCN)NC([C@@H](NC([C@@H](NC([C@@H]3CCCN3C([C@@H](NC([C@@H](NC([C@H](CCCNC(N)=N)NC([C@H](CC(C)C)NC([C@@H]4CCCN4C([C@H](CO)NC([C@@H](NC([C@@H](NC([C@H](CO)NC([C@@H](NC([C@@H](NC(CNC(C)=O)=O)CC(O)=O)=O)CC5=CC=C(O)C=C5)=O)=O)CC6=CN=CN6)=O)CS)=O)=O)=O)=O)=O)CC7=CC=C(O)C=C7)=O)CC8=CC=C(O)C=C8)=O)=O)CC9=CNC%10=C9C=CC=C%10)=O)CC%11=CNC%12=C%11C=CC=C%12)=O)=O)CS)=O)=O)CC%13=CC=C(O)C=C%13)=O)=O)CC(O)=O)=O)=O)=O)=O)=O)=O.OC(C(F)(F)F)=O
InChi Code
InChI=1S/C141H187N35O40S2.C2HF3O2/c1-72(2)50-93(163-133(209)109-24-15-49-176(109)140(216)104(68-178)169-130(206)105(69-217)171-127(203)98(57-81-62-146-71-154-81)162-129(205)103(67-177)168-124(200)95(52-76-28-36-83(182)37-29-76)160-128(204)99(58-116(191)192)155-114(188)66-148-74(4)180)122(198)157-91(21-11-45-147-141(144)145)120(196)159-94(51-75-26-34-82(181)35-27-75)123(199)165-100(53-77-30-38-84(183)39-31-77)137(213)173-46-13-23-108(173)134(210)164-97(56-80-61-150-89-19-8-6-17-87(80)89)126(202)161-96(55-79-60-149-88-18-7-5-16-86(79)88)125(201)156-90(20-9-10-44-142)121(197)170-106(70-218)131(207)172-118(73(3)179)136(212)167-101(54-78-32-40-85(184)41-33-78)138(214)174-47-14-25-110(174)135(211)166-102(59-117(193)194)139(215)175-48-12-22-107(175)132(208)158-92(42-43-115(189)190)119(195)153-65-113(187)152-64-112(186)151-63-111(143)185;3-2(4,5)1(6)7/h5-8,16-19,26-41,60-62,71-73,90-110,118,149-150,177-179,181-184,217-218H,9-15,20-25,42-59,63-70,142H2,1-4H3,(H2,143,185)(H,146,154)(H,148,180)(H,151,186)(H,152,187)(H,153,195)(H,155,188)(H,156,201)(H,157,198)(H,158,208)(H,159,196)(H,160,204)(H,161,202)(H,162,205)(H,163,209)(H,164,210)(H,165,199)(H,166,211)(H,167,212)(H,168,200)(H,169,206)(H,170,197)(H,171,203)(H,172,207)(H,189,190)(H,191,192)(H,193,194)(H4,144,145,147);(H,6,7)/t73-,90+,91+,92+,93+,94+,95+,96+,97+,98+,99+,100+,101+,102+,103+,104+,105+,106+,107+,108+,109+,110+,118+;/m1./s1
InChi Key
VIFRSXGPENFSMZ-OZZMATMRSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $395

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    1 mg

    $751

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    Product Description

    DX600 is a potent and selective peptide inhibitor of angiotensin-converting enzyme 2 (ACE2; Kis = 2.8, 200, and 1,200 nM for recombinant, human, and murine ACE2, respectively).1,2 ACE2 is an enzyme that is cardioprotective and renoprotective.3 Inhibition of ACE2 with DX600 reduces in vitro vascular repair by CD34+ stem/progenitor cells and exacerbates myocardial injury and dysfunction in vivo.4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Huang, L., Sexton, D.J., Skogerson, K., et al. Novel peptide inhibitors of angiotensin-converting enzyme 2. The Journal of Biological Chemisty 278(18), 15532-15540 (2003).

    2. Joshi, S., Balasubramanian, N., Vasam, G., et al. Angiotensin converting enzyme versus angiotensin converting enzyme-2 selectivity of MLN-4760 and DX600 in human and murine bone marrow-derived cells. Eur. J. Pharmacol. 774, 25-33 (2016).

    3. Prada, J.A.H., Ferreira, A.J., Katovich, M.J., et al. Structure-based identification of small-molecule angiotensin-converting enzyme 2 activators as novel antihypertensive agents. Hypertension 51, 1312-1317 (2008).

    4. Singh, N., Joshi, S., Guo, L., et al. ACE2/Ang-(1-7)/Mas axis stimulates vascular repair-relevant functions of CD34+ cells. Am. J. Physiol. Heart. Circ. Physiol. 309, H1697-H1707 (2015).

    5. Song, B., Zhang, Z.-Z., Zhong, J.-C., et al. Loss of angiotensin-converting enzyme 2 exacerbates myocardial injury via activation of the CTGF-fractalkine signaling pathway. Circ. J. 77(12), 2997-3006 (2013).