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PACAP 6-38

Alias: PACAP (6-38), human, ovine, rat
Cat No.:V2753 Purity: ≥98%
COA Product Data Instructions for use SDS
PACAP 6-38 is a novel and potent PACAP (pituitary adenylate cyclase-activating polypeptide) non-stimulating competitive antagonist with an IC50 value of 2 nM.
PACAP 6-38
PACAP 6-38 Chemical Structure CAS No.: 143748-18-9
Product category: cAMP
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

COA
MSDS
Instructions
Product Description

PACAP 6-38 is a novel and potent PACAP (pituitary adenylate cyclase-activating polypeptide) non-stimulating competitive antagonist with an IC50 value of 2 nM. It acts as a functional CARTp antagonist in vivo. It also prevents differentiated cells' ERK from being phosphorylated by CARTp. When the PAC1 receptor antagonist PACAP(6-38) (300 nM) was administered intravenously to NGF-OE mice, the intercontraction interval (2.0-fold) and void volume (2.5-fold) increased significantly (p ≤ 0.01). In NGF-OE mice, intravesical administration of PACAP(6-38) also reduced baseline bladder pressure. In WT mice, PACAP(6-38) had no effect on bladder function. When administered intravenously, 300 nM of PACAP(6-38) significantly (p ≤ 0.01) decreased pelvic sensitivity in NGF-OE mice, but had no effect on WT mice. The increased frequency of voiding and increased sensitivity to the pelvis seen in NGF-OE mice can be attributed to PACAP/receptor signaling.

Biological Activity I Assay Protocols (From Reference)
Targets
PACAP type I receptor ( IC50 = 30 nM ); PACAP type II receptor VIP1 ( IC50 = 600 nM ); PACAP type II receptor VIP2 ( IC50 = 40 nM )
ln Vitro

In vitro activity: ACAP 6-38 is a novel and potent PACAP (pituitary adenylate cyclase-activating polypeptide) non-stimulating competitive antagonist with an IC50 value of 2 nM. It acts as a functional CARTp antagonist in vivo. Additionally, in differentiated cells, it prevents the phosphorylation of ERK induced by CARTp. When NGF-OE mice were given the PAC1 receptor antagonist PACAP(6-38) (300 nM) intravenously, their intercontraction interval (which increased by 2.0 times) and void volume (which increased by 2.5 times) were both significantly (p ≤ 0.01) higher. In addition, intravesical administration of PACAP(6-38) reduced the NGF-OE mice's baseline bladder pressure. WT mice's bladder function was unaffected by PACAP(6-38). Intravesical administration of 300 nM PACAP(6-38) reduced pelvic sensitivity in NGF-OE mice significantly (p ≤ 0.01), but had no effect on WT mice. The increased frequency and sensitivity of the pelvic area seen in NGF-OE mice during voiding is partly explained by PACAP/receptor signaling.
ln Vivo
NGF-OE mice exhibit a significant (p ≤ 0.01) increase in intercontraction interval (2.0-fold) and void volume (2.5-fold) upon intravesical administration of PACAP(6-38) (300 nM), an antagonist of the PAC1 receptor. On bladder function in WT mice, PACAP(6-38) has no effect. Pelvic sensitivity is significantly (p ≤ 0.01) reduced in NGF-OE mice after intravesical administration of 300 nM PACAP(6-38), but not in WT mice.
Enzyme Assay
PACAP (6-38), human, ovine, and rat is a strong antagonist of PACAP receptors, with IC50 values for PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2 of 30, 600, and 40 nM, respectively.
Cell Assay
In the presence or absence of the PACAP antagonist PACAP (6-38), cells are incubated with 300 nM PACAP-38 for 4 hours. The medium is then collected, and proteins are separated via SDS/PAGE and blotted onto PVDF membranes. Membranes are probed with antibody 6E10, then an anti-mouse antibody labeled with HRP is applied. The ECL plus system is used to detect APPsα.
Animal Protocol
0.9% saline;0.3 nmol, 0.6 nmol, 3 nmol (1.5 Μl/340g);i.c.v
Male Sprague-Dawley rats
References

[1]. Eur J Biochem . 1992 Jul 1;207(1):239-46.

[2]. PLoS One . 2013 Aug 15;8(8):e72347.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C182H300N56O45S
Molecular Weight
4024.74259999997
Exact Mass
4023.27
CAS #
143748-18-9
Related CAS #
PACAP (6-38), human, ovine, rat TFA
PubChem CID
24868185
Appearance
Typically exists as solid at room temperature
LogP
-11.8
Hydrogen Bond Donor Count
64
Hydrogen Bond Acceptor Count
58
Rotatable Bond Count
146
Heavy Atom Count
284
Complexity
9190
Defined Atom Stereocenter Count
33
SMILES
C[C@H]([C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC3=CC=C(C=C3)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC4=CC=C(C=C4)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CCCCN)C(=O)N)NC(=O)[C@H](CC5=CC=CC=C5)N)O
InChi Key
BGZYREVJBMQLGS-ONKNJJKASA-N
InChi Code
InChI=1S/C182H300N56O45S/c1-95(2)83-128(152(257)207-92-141(249)211-115(40-20-27-72-184)154(259)215-122(47-34-79-204-180(197)198)161(266)226-130(86-105-50-58-109(242)59-51-105)167(272)217-117(42-22-29-74-186)156(261)220-125(66-68-138(191)246)163(268)216-124(49-36-81-206-182(201)202)165(270)237-145(99(9)10)176(281)224-120(45-25-32-77-189)160(265)230-134(90-140(193)248)171(276)212-114(147(194)252)39-19-26-71-183)231-177(282)144(98(7)8)236-149(254)101(12)208-148(253)100(11)210-166(271)129(84-96(3)4)225-169(274)132(88-107-54-62-111(244)63-55-107)228-159(264)118(43-23-30-75-187)214-157(262)119(44-24-31-76-188)223-175(280)143(97(5)6)235-150(255)102(13)209-153(258)127(70-82-284-15)222-164(269)126(67-69-139(192)247)221-155(260)116(41-21-28-73-185)213-158(263)121(46-33-78-203-179(195)196)218-168(273)131(87-106-52-60-110(243)61-53-106)227-162(267)123(48-35-80-205-181(199)200)219-173(278)136(93-239)233-170(275)133(89-108-56-64-112(245)65-57-108)229-174(279)137(94-240)234-172(277)135(91-142(250)251)232-178(283)146(103(14)241)238-151(256)113(190)85-104-37-17-16-18-38-104/h16-18,37-38,50-65,95-103,113-137,143-146,239-245H,19-36,39-49,66-94,183-190H2,1-15H3,(H2,191,246)(H2,192,247)(H2,193,248)(H2,194,252)(H,207,257)(H,208,253)(H,209,258)(H,210,271)(H,211,249)(H,212,276)(H,213,263)(H,214,262)(H,215,259)(H,216,268)(H,217,272)(H,218,273)(H,219,278)(H,220,261)(H,221,260)(H,222,269)(H,223,280)(H,224,281)(H,225,274)(H,226,266)(H,227,267)(H,228,264)(H,229,279)(H,230,265)(H,231,282)(H,232,283)(H,233,275)(H,234,277)(H,235,255)(H,236,254)(H,237,270)(H,238,256)(H,250,251)(H4,195,196,203)(H4,197,198,204)(H4,199,200,205)(H4,201,202,206)/t100-,101-,102-,103+,113-,114-,115-,116-,117-,118-,119-,120-,121-,122-,123-,124-,125-,126-,127-,128-,129-,130-,131-,132-,133-,134-,135-,136-,137-,143-,144-,145-,146-/m0/s1
Chemical Name
(3S)-4-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-[[(2S,3R)-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-4-oxobutanoic acid
Synonyms
PACAP (6-38), human, ovine, rat
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 Data
Solubility (In Vitro)
DMSO: N/A
Water: ~100 mg/mL (24.84 mM)
Ethanol: N/A
Solubility (In Vivo)
N/A
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 0.2485 mL 1.2423 mL 2.4846 mL
5 mM 0.0497 mL 0.2485 mL 0.4969 mL
10 mM 0.0248 mL 0.1242 mL 0.2485 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.

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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.
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Biological Data

  • PACAP 6-38

    Summary histogram of bladder pressure (BP) measured from bladder function testing in WT (n = 8) and NGF-OE (n = 8) before and after intravesical instillation of PACAP(6–38) (300 NM).2016 Jun;59(2):290-9.

  • An external file that holds a picture, illustration, etc. Object name is nihms842760f4.jpg

    Summary histogram of the number of non-voiding contractions (NVCs) measured from bladder function testing in WT (n = 8) and NGF-OE (n = 8) before and after intravesical instillation of PACAP(6–38) (300 nM).2016 Jun;59(2):290-9.

  • An external file that holds a picture, illustration, etc. Object name is nihms842760f5.jpg

    Pelvic region testing with calibrated von Frey hairs was determined in WT and NGF-OE mice.2016 Jun;59(2):290-9.
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